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2-(Piperidin-3-yl)phthalimides reduce classical markers of cellular inflammation in LPS-challenged RAW 264.7 cells and also demonstrate potentially relevant sigma and serotonin receptor affinity in membrane preparations.
Bioorg Med Chem Lett 110:
National Institute on Aging
Plakevulin A induces apoptosis and suppresses IL-6-induced STAT3 activation in HL60 cells.
Bioorg Med Chem Lett 110:
Tokyo University of Science
N-methylmorpholine incorporation into the structure of biphenyl leads to the bioactive inhibitor of PD-1/PD-L1 interaction.
Bioorg Med Chem Lett 110:
Jagiellonian University
Structure-based discovery of novel piperidine-biphenyl-DAPY derivatives as non-nucleoside reverse transcriptase inhibitors featuring improved potency, safety, and selectivity: From piperazine-biphenyl-DAPYs to piperidine-biphenyl-DAPYs.
Eur J Med Chem 276:
Fudan University
Targeting prolidase. A survey of the literature data to depict a structure-activity relationship frame and to address future studies for drug development.
Bioorg Med Chem 110:
Universita "Gabriele d'Annunzio" Chieti - Pescara
The Development of a Highly Potent and Selective Human Toll-like Receptor 2 Agonist: Synthesis and Biological Evaluation of CaLGL-1 and Its Derivatives.
J Med Chem 67: 12932-12944
Lanzhou University
Discovery of Novel Diaryl-Substituted Fused Heterocycles Targeting Katanin and Tubulin with Potent Antitumor and Antimultidrug Resistance Efficacy.
J Med Chem 67: 12118-12142
Fudan University
Amphiphilic Heparinoids as Potent Antiviral Agents against SARS-CoV-2.
J Med Chem 67: 11885-11916
University of Queensland
Targeting Myeloperoxidase Ameliorates Gouty Arthritis: A Virtual Screening Success Story.
J Med Chem 67: 12012-12032
University of Sao Paulo
Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches.
J Med Chem 67: 10530-10547
Hebei University of Science & Technology
Discovery of N'-benzyl-3-chloro-N-((1S,3R,4R)-3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)cyclohexyl)benzenesulfonamide as a novel selective KOR ligand.
Eur J Med Chem 276:
Fudan University
Structure-based mapping of the histone-binding pocket of KDM4D using functionalized tetrazole and pyridine core compounds.
Eur J Med Chem 276:
Max-Delbruck-Center for Molecular Medicine
Structure-activity relationships of middle-size cyclic peptides, KRAS inhibitors derived from an mRNA display.
Bioorg Med Chem 110:
Chugai Pharmaceutical Co. Ltd.
Synthesis, biosimulation and pharmacological evaluation of benzimidazole derivatives with antihypertensive multitarget effect.
Bioorg Med Chem Lett 110:
Universidad Autonoma del Estado de Morelos
Design, synthesis and structure-activity relationships of novel non-ketolides: 9-Oxime clarithromycin featured with seven-to thirteen-atom-length diamine linkers at 3-OH.
Eur J Med Chem 276:
Beijing Institute of Technology
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists.
Eur J Med Chem 276:
University of North Carolina at Chapel Hill
Synthesis and evaluation of neuroactive steroids with novel pharmacophore at C-21 let identify a compound with advantageous PK profile and higher EC50 and Emax as PAM on GABAA receptor.
Eur J Med Chem 276:
Yantai University
Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension.
J Med Chem 67: 16128-16144
China Pharmaceutical University
New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs.
J Med Chem 67: 11522-11542
China Pharmaceutical University
Synthesis and activity of benzimidazole N-Acylhydrazones against Trypanosoma cruzi, Leishmania amazonensis and Leishmania infantum.
Bioorg Med Chem Lett 110:
Instituto de Tecnologia em Farmacos
Design and synthesis of 7-membered lactam fused hydroxypyridinones as potent metal binding pharmacophores (MBPs) for inhibiting influenza virus PAN endonuclease.
Eur J Med Chem 276:
Zhejiang University
Research progress of multi-target HDAC inhibitors blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway in the treatment of cancer.
Bioorg Med Chem 110:
Jincheng People's Hospital
Targeting Relevant HDACs to Support the Survival of Cone Photoreceptors in Inherited Retinal Diseases: Identification of a Potent Pharmacological Tool with In Vitro and In Vivo Efficacy.
J Med Chem 67: 14946-14973
University of Siena
A Diterpenoid of the Medicinal Plant Andrographis paniculata Targets Cutaneous TRPV3 Channel and Relieves Itch.
J Nat Prod 87: 1852-1859
Russian Academy of Sciences
NN1213 - A Potent, Long-Acting, and Selective Analog of Human Amylin.
J Med Chem 67: 11688-11700
Novo Nordisk A/S
Recent progress in the development of hypoxia-inducible factor 2α (HIF-2α) modulators: Inhibitors, agonists, and degraders (2009-2024).
Eur J Med Chem 275:
Hubei Polytechnic University
Design, synthesis, pharmacological evaluation, and computational study of benzo[d] isothiazol-based small molecule inhibitors targeting PD-1/PD-l1 interaction.
Eur J Med Chem 275:
Shenyang Pharmaceutical University
Binding sites and design strategies for small molecule GLP-1R agonists.
Eur J Med Chem 275:
China Pharmaceutical University
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
J Med Chem 67: 12261-12313
University of North Carolina at Chapel Hill
Lipid Trolling to Optimize A3 Adenosine Receptor-Positive Allosteric Modulators (PAMs).
J Med Chem 67: 12221-12247
National Institute of Diabetes and Digestive and Kidney Diseases
Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy.
J Med Chem 67: 11917-11936
Nanjing University of Chinese Medicine
New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives.
J Med Chem 67: 11488-11521
University of Bologna
An overview of RAF kinases and their inhibitors (2019-2023).
Eur J Med Chem 275:
University of Sharjah
Structure-Guided Design of Potent Coronavirus Inhibitors with a 2-Pyrrolidone Scaffold: Biochemical, Crystallographic, and Virological Studies.
J Med Chem 67: 11937-11956
Wichita State University
Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8.
J Med Chem 67: 12784-12806
University of Florida
Discovery of GPR84 Fluorogenic Probes Based on a Novel Antagonist for GPR84 Bioimaging.
J Med Chem 67: 10875-10890
Chinese Academy of Sciences
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance.
Eur J Med Chem 275:
Southwest University
PepExplainer: An explainable deep learning model for selection-based macrocyclic peptide bioactivity prediction and optimization.
Eur J Med Chem 275:
Zhejiang University
Synthesis of thiazolidine-2,4-dione tethered 1,2,3-triazoles as α-amylase inhibitors: In vitro approach coupled with QSAR, molecular docking, molecular dynamics and ADMET studies.
Eur J Med Chem 275:
Kurukshetra University
Development of Degraders of Cyclin-Dependent Kinases 4 and 6 Based on Rational Drug Design.
J Med Chem 67: 11354-11364
East China Normal University
Discovery of Oxidized p-Terphenyls as Phosphodiesterase 4 Inhibitors from Marine-Derived Fungi.
J Nat Prod 87: 1808-1816
Chinese Academy of Sciences
Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity.
Bioorg Med Chem Lett 110:
University of Dundee
Design and synthesis of novel and potent allosteric HIV-1 integrase inhibitors with a spirocyclic moiety.
Bioorg Med Chem Lett 110:
Japan Tobacco
Skin- and airway-deliverable TRPA1 inhibitor.
Bioorg Med Chem 110:
Kao Corporation
Development of novel antivrial agents that induce the degradation of the main protease of human-infecting coronaviruses.
Eur J Med Chem 275:
Chinese Academy of Sciences
5-HT6 receptor neutral antagonists protect astrocytes: A lesson from 2-phenylpyrrole derivatives.
Eur J Med Chem 275:
Jagiellonian University Medical College
Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β-Glucocerebrosidase.
J Med Chem 67: 11168-11181
Astex Pharmaceuticals
Machine learning-based QSAR and LB-PaCS-MD guided design of SARS-CoV-2 main protease inhibitors.
Bioorg Med Chem Lett 110:
Chulalongkorn University
Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease.
Eur J Med Chem 275:
Northwest A&F University
Lipid-conjugated nucleoside monophosphate and monophosphonate prodrugs: A versatile drug delivery paradigm.
Eur J Med Chem 275:
Xichang University
Synthesis and biological characterization of an orally bioavailable lactate dehydrogenase-A inhibitor against pancreatic cancer.
Eur J Med Chem 275:
Southwestern Oklahoma State University
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
J Med Chem 67: 10548-10566
Kymera Therapeutics
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma.
J Med Chem 67: 10743-10773
China Pharmaceutical University
Revisiting the antiangiogenic mechanisms of fluorinated thalidomide derivatives.
Bioorg Med Chem Lett 110:
University of Bonn
Modulation of endogenous opioid signaling by inhibitors of puromycin-sensitive aminopeptidase.
Eur J Med Chem 275:
University of Minnesota
Macrocarpal B blocks the binding between the phospholipase A2 receptor and its antibodies.
Bioorg Med Chem 110:
Peking University First Hospital
Development of a Potent and Selective G2A (GPR132) Agonist.
J Med Chem 67: 10567-10588
Fraunhofer Institute for Translational Medicine and Pharmacology ITMP
Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1.
J Med Chem 67: 11209-11225
AstraZeneca
Structure-based development of novel substrate-type G9a inhibitors as epigenetic modulators for sickle cell disease treatment.
Bioorg Med Chem Lett 110:
Kyorin Pharmaceutical Co. Ltd.
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
J Med Chem 67: 10795-10830
University of Chinese Academy of Sciences
Fragment-Based Anti-inflammatory Agent Design and Target Identification: Discovery of AF-45 as an IRAK4 Inhibitor to Treat Ulcerative Colitis and Acute Lung Injury.
J Med Chem 67: 10687-10709
Wenzhou Medical University
Discovery of Novel Receptor Tyrosine Kinase-like Orphan Receptor 1 (ROR1) Inhibitors for Cancer Treatment.
J Med Chem 67: 10655-10686
Sichuan University
Discovery of Highly Selective, Potent, Covalent, and Orally Bioavailable Factor XIIa Inhibitors for the Treatment of Thrombo-Inflammation.
J Med Chem 67: 10946-10966
Hefei University of Technology
Discovery of Dual MER/AXL Kinase Inhibitors as Bifunctional Small Molecules for Inhibiting Tumor Growth and Enhancing Tumor Immune Microenvironment.
J Med Chem 67: 10906-10927
National Health Research Institutes
Discovery of Novel 1-Phenylpiperidine Urea-Containing Derivatives Inhibiting β-Catenin/BCL9 Interaction and Exerting Antitumor Efficacy through the Activation of Antigen Presentation of cDC1 Cells.
J Med Chem 67: 12485-12520
Anhui University of Chinese Medicine
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein.
RSC Med Chem 15: 1942-1958
Indoan Institute of Technology
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches.
RSC Med Chem 15: 2146-2159
Johannes Gutenberg University
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold.
RSC Med Chem 15: 1798-1827
Monash University
Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update.
RSC Med Chem 15: 1877-1898
American University of Ras Al Khaimah
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure-activity relationship and molecular docking studies (2018-2024).
RSC Med Chem 15: 1849-1876
ISF College of Pharmacy Ghal Kalan
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity.
RSC Med Chem 15: 1929-1941
Sinop University
Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents.
RSC Med Chem 15: 2080-2097
King Faisal University
Amine-containing donepezil analogues as potent acetylcholinesterase inhibitors with increased polarity.
RSC Med Chem 15: 2037-2044
University of New South Wales
Discovery of aurones bearing two amine functionalities as SHIP2 inhibitors with insulin-sensitizing effect in rat myotubes.
RSC Med Chem 15: 2179-2195
Universiti Sains Malaysia
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer.
RSC Med Chem 15: 2045-2062
University of Bologna
Small molecule targeted therapies for endometrial cancer: progress, challenges, and opportunities.
RSC Med Chem 15: 1828-1848
Yixing People's Hospital Yixing
Discovery of new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation.
Eur J Med Chem 275:
Sun Yat-sen University
Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor.
Eur J Med Chem 275:
Sichuan University
Novel dihydropyrimidines as promising EGFR & HER2 inhibitors: Insights from experimental and computational studies.
Eur J Med Chem 275:
JSS College of Pharmacy
Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation.
J Med Chem 67: 11103-11124
Chiesi Farmaceutici S.p.A
Structure-activity relationship of dual inhibitors containing maleimide and imidazole motifs against glutaminyl cyclase and glycogen synthase kinase-3β.
Bioorg Med Chem Lett 110:
Shenzhen University Medical School
Exploring the interaction of N-(benzothiazol-2-yl)pyrrolamide DNA gyrase inhibitors with the GyrB ATP-binding site lipophilic floor: A medicinal chemistry and QTAIM study.
Bioorg Med Chem 109:
University of Ljubljana
Optimization of α-amido boronic acids via cryo-electron microscopy analysis: Discovery of a novel highly selective immunoproteasome subunit LMP7 (β5i)/LMP2 (β1i) dual inhibitor.
Bioorg Med Chem 109:
Mitsubishi Tanabe Pharma Corporation
Discovery of novel pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione (PBD) derivatives as selective HDAC6 inhibitors for the efficient treatment of idiopathic pulmonary fibrosis (IPF) in vitro and in vivo.
Eur J Med Chem 275:
Shenyang Pharmaceutical University
Discovery of 5-(Piperidin-4-yl)-1,2,4-oxadiazole Derivatives as a New Class of Human Caseinolytic Protease P Agonists for the Treatment of Hepatocellular Carcinoma.
J Med Chem 67: 10622-10642
Sichuan University
Rational Molecular Editing: A New Paradigm in Drug Discovery.
J Med Chem 67: 11459-11466
Henan Normal University
Design, synthesis and antibacterial activity evaluation of ebselen derivatives in NDM-1 producing bacteria.
RSC Med Chem 15: 1959-1972
Ocean University of China
Dual 5-HT6/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.
Eur J Med Chem 275:
Jagiellonian University Medical College
Extensive targeting of chemical space at the prime side of ketoamide inhibitors of rhomboid proteases by branched substituents empowers their selectivity and potency.
Eur J Med Chem 275:
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Science
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis.
J Med Chem 67: 10710-10742
Julius-Maximilians-Universitat Wurzburg (JMU)
Discovery of novel natural-product-derived mutant isocitrate dehydrogenases 1 inhibitors: Structure-based virtual screening, biological evaluation and structure-activity relationship study.
Eur J Med Chem 275:
Chongqing Medical University
G Protein-Coupled Estrogen Receptor-Mediated Anti-Inflammatory and Mucosal Healing Activity of a Trimethylpyridinol Analogue in Inflammatory Bowel Disease.
J Med Chem 67: 10601-10621
Yeungnam University
Potent, Selective, and Orally Bioavailable Quinazoline-Based STK17A/B Dual Inhibitors.
ACS Med Chem Lett 15: 945-949
University of Miami Miller School of Medicine
Novel HSD17B13 Inhibitors for Treating Liver Diseases.
ACS Med Chem Lett 15: 771-772
Smith, Gambrell & Russell
2-Aminopyridines as Potent and Selective Nav1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model.
ACS Med Chem Lett 15: 917-923
Merck & Co.
Novel 2,4-Dichloro-5-sulfamoylbenzoic Acid Oxime Esters: First Studies as Potential Human Carbonic Anhydrase Inhibitors.
ACS Med Chem Lett 15: 972-978
MGM University
Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding.
ACS Med Chem Lett 15: 864-872
Genentech
Benzodioxane Carboxamide Derivatives As Novel Monoamine Oxidase B Inhibitors with Antineuroinflammatory Activity.
ACS Med Chem Lett 15: 798-805
Zunyi Medical University
Lead Identification of Novel Naphthyridine Derivatives as Potent SOS1 Inhibitors.
ACS Med Chem Lett 15: 958-964
Haihe Biopharma Co., Ltd.
Lysosomal Degradation of Extracellular Targets: Innovations and Implications.
ACS Med Chem Lett 15: 752-754
Usona Institute
Structure-Based Rational Design of Constrained Peptides as TIM-3 Inhibitors.
ACS Med Chem Lett 15: 806-813
Weill Cornell Medicine
Structural Modifications of Covalent Cathepsin S Inhibitors: Impact on Affinity, Selectivity, and Permeability.
ACS Med Chem Lett 15: 837-844
Johannes Gutenberg University Mainz
Novel Heteroaryl Compounds as CD73 Inhibitors for Treating Cancer.
ACS Med Chem Lett 15: 775-776
Smith, Gambrell & Russell
Nonsymmetrically Substituted 1,1'-Biphenyl-Based Small Molecule Inhibitors of the PD-1/PD-L1 Interaction.
ACS Med Chem Lett 15: 828-836
Jagiellonian University
The Inhibitors of Mucosa-Associated Lymphoid Tissue Lymphoma Translocation Protein 1 (MALT-1) Protease as Potential Treatment of ABC-DLBCL and Similar Diseases.
ACS Med Chem Lett 15: 763-765
PI Health Sciences
SARS-CoV-2 Main Protease Inhibitors That Leverage Unique Interactions with the Solvent Exposed S3 Site of the Enzyme.
ACS Med Chem Lett 15: 950-957
Texas A&M University
Imidazopyridine Compounds as ERK5 Inhibitors for Treating Cancer.
ACS Med Chem Lett 15: 777-778
Smith Gambrell & Russell LLP
Novel 2,7-Naphthyridine Compounds as MASTL Inhibitors for Treating Cancer.
ACS Med Chem Lett 15: 748-749
Smith, Gambrell & Russell
Insight on Some Newly Synthesized Trisubstituted Imidazolinones as VEGFR-2 Inhibitors.
ACS Med Chem Lett 15: 892-898
Cairo University
Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen.
ACS Med Chem Lett 15: 791-797
AstraZeneca
The U.S. FDA approved cardiovascular drugs from 2011 to 2023: A medicinal chemistry perspective.
Eur J Med Chem 275:
Sichuan University
Novel carbazole-oxadiazole derivatives as anti-α-glucosidase and anti-α-amylase agents: Design, synthesis, molecular docking, and biological evaluation.
Eur J Med Chem 275:
Guizhou Medical University
Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors.
Eur J Med Chem 275:
Shenyang Pharmaceutical University
Discovery of JNJ-74856665: A Novel Isoquinolinone DHODH Inhibitor for the Treatment of AML.
J Med Chem 67: 11254-11272
Janssen Research and Development
Discovery of Novel Proteolysis-Targeting Chimera Molecules as Degraders of Programmed Cell Death-Ligand 1 for Breast Cancer Therapy.
J Med Chem 67: 10589-10600
Sichuan University
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
J Med Chem 67: 10831-10847
Pfizer
Design, Synthesis, and Activity Evaluation of Novel Benzazole Bifunctional Antifungal Inhibitors with an LDH Carrier.
J Med Chem 67: 11365-11388
Liaocheng University
Discovery of a Novel ASM Direct Inhibitor with a 1,5-Diphenyl-pyrazole Scaffold and Its Antidepressant Mechanism of Action.
J Med Chem 67: 10350-10373
China Pharmaceutical University
Discovery and Development of NLRP3 Inhibitors Targeting the LRR Domain to Disrupt NLRP3-NEK7 Interaction for the Treatment of Rheumatoid Arthritis.
J Med Chem 67: 9869-9895
China Pharmaceutical University
Discovery of novel CXCR4 inhibitors for the treatment of inflammation by virtual screening and biological evaluation.
Eur J Med Chem 275:
Anhui Medical University
Potent, Selective Agonists for the Cannabinoid-like Orphan G Protein-Coupled Receptor GPR18: A Promising Drug Target for Cancer and Immunity.
J Med Chem 67: 9896-9926
University of Bonn
Discovery of Orally Bioavailable and Potent CDK9 Inhibitors for Targeting Transcription Regulation in Triple-Negative Breast Cancer.
J Med Chem 67: 10035-10056
University of Chinese Academy of Sciences
Exploring the structural activity relationship of the Osimertinib: A covalent inhibitor of double mutant EGFRL858R/T790M tyrosine kinase for the treatment of Non-Small Cell Lung Cancer (NSCLC).
Bioorg Med Chem 109:
R. C. Patel Institute of Pharmaceutical Education and Research
Development and therapeutic perspectives of CXCR4 antagonists for disease therapy.
Eur J Med Chem 275:
Sichuan University
Discovery of pyridazinone derivatives bearing tetrahydroimidazo[1,2-a]pyrazine scaffold as potent inhibitors of transient receptor potential canonical 5 to ameliorate hypertension-induced renal injury in rats.
Eur J Med Chem 275:
Nanjing University of Chinese Medicine
Design and synthesis of 6-C-alkyl-DMDP type nanomolar inhibitors of β-galactosidase and β-glucosidase based on broussonetine S and related derivatives.
Eur J Med Chem 275:
Beijing National Laboratory For Molecular Sciences
Discovery of new anti-diabetic potential agents based on paracetamol incorporating sulfa-drugs: Design, synthesis, α-amylase, and α-glucosidase inhibitors with molecular docking simulation.
Eur J Med Chem 275:
Northern Border University
Discovery of a potent orally available pyrazolopyridone derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor.
Bioorg Med Chem Lett 109:
Mitsubishi Tanabe Pharma Corporation
Discovery of a potent, orally available furopyridine derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor.
Bioorg Med Chem Lett 109:
Mitsubishi Tanabe Pharma Corporation
Synthesis and biological evaluation of multimodal monoaminergic arylpiperazine derivatives with potential antidepressant profile.
Eur J Med Chem 275:
University of Chinese Academy of Sciences
Novel thiosemicarbazide-based β-carboline derivatives as α-glucosidase inhibitors: Synthesis and biological evaluation.
Eur J Med Chem 275:
Wuyi University
Discovery of N-Substituted Acetamide Derivatives as Promising P2Y14R Antagonists Using Molecular Hybridization Based on Crystallographic Overlay.
J Med Chem 67: 10233-10247
Children's Hospital Affiliated to Zhengzhou University
Design, Synthesis, and Biological Evaluation of 1,2,4-Oxadiazole Derivatives Containing an Aryl Carboxylic Acid Moiety as Potent Sarbecovirus Papain-like Protease Inhibitors.
J Med Chem 67: 10211-10232
Peking Union Medical College and Chinese Academy of Medical Sciences
An insight into sustainable and green chemistry approaches for the synthesis of quinoline derivatives as anticancer agents.
Eur J Med Chem 275:
Acharya & BM Reddy College of Pharmacy
Discovery of autophagy-tethering compounds as potent NLRP3 degraders for IBD Immunotherapy.
Eur J Med Chem 275:
Fudan University
Bioisosteric heterocyclic analogues of natural bioactive flavonoids by scaffold-hopping approaches: State-of-the-art and perspectives in medicinal chemistry.
Bioorg Med Chem 109:
University of Palermo
Efficient synthesis of indole-chalcones based glycohybrids and their anticancer activity.
Bioorg Med Chem 109:
Jawaharlal Nehru University
Fentanyl-Type Antagonist of the μ-Opioid Receptor: Important Role of Axial Chirality in the Active Conformation.
J Med Chem 67: 10447-10463
Tokyo University of Science
Exploration of 1-(indolin-1-yl)-2-(thiazol-2-yl)ethan-1-one derivatives as novel anti-HBV agent with potential TLR7-agonistic effect.
Eur J Med Chem 275:
Xuzhou Medical University
A chemical modification of a peroxisome proliferator-activated receptor pan agonist produced a shift to a new dual alpha/gamma partial agonist endowed with mitochondrial pyruvate carrier inhibition and antidiabetic properties.
Eur J Med Chem 275:
Universita degli Studi di Bari "Aldo Moro"
Synthetically Feasible De Novo Molecular Design of Leads Based on a Reinforcement Learning Model: AI-Assisted Discovery of an Anti-IBD Lead Targeting CXCR4.
J Med Chem 67: 10057-10075
Hangzhou Normal University
Discovery of 7-alkoxybenzofurans as PDE4 inhibitors with hepatoprotective activity in D-GalN/LPS-induced hepatic sepsis.
Eur J Med Chem 275:
NMPA Key Laboratory for Research and Evaluation of Drug Metabolism & Guangdong Provinc
Advances in dual-targeting inhibitors of HDAC6 for cancer treatment.
Eur J Med Chem 275:
Guizhou Medical University
Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine.
J Med Chem 67: 10135-10151
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
Identification and Validation of PKR as a Direct Target for the Novel Sulfonamide-Substituted Tetrahydroquinoline Nonselective Inhibitor of the NLRP3 Inflammasome.
J Med Chem 67: 10168-10189
China Pharmaceutical University
Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity.
Eur J Med Chem 275:
Shenyang Pharmaceutical University
Non-kinase off-target inhibitory activities of clinically-relevant kinase inhibitors.
Eur J Med Chem 275:
Purdue University
New insights into butyrylcholinesterase: Pharmaceutical applications, selective inhibitors and multitarget-directed ligands.
Eur J Med Chem 275:
China Pharmaceutical University
[1,2,4]Triazolo[1,5-a]pyrimidine derivatives: Structure-activity relationship study leading to highly selective ENPP1 inhibitors.
Bioorg Med Chem Lett 110:
Nagoya City University
Psammaplin A analogues with modified disulfide bond targeting histone deacetylases: Synthesis and biological evaluation.
Eur J Med Chem 275:
Ocean University of China
Identification of sulfonylpyrimidines as novel selective aldosterone synthase (CYP11B2) inhibitors.
Bioorg Med Chem 108:
Daiichi Sankyo Co., Ltd.
Design, synthesis, biological evaluation, and in silico studies of novel pyridopyridine derivatives as anticancer candidates targeting FMS kinase.
Eur J Med Chem 274:
University of Sharjah
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
J Med Chem 67: 10248-10262
Pfizer
Structure-Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD+-Dependent Lysine Deacylase Sirtuin 2.
J Med Chem 67: 10076-10095
University of Freiburg
Advanced Design, Synthesis, and Evaluation of Highly Selective Wee1 Inhibitors: Enhancing Pharmacokinetics and Antitumor Efficacy.
J Med Chem 67: 9927-9949
China Pharmaceutical University
Discovery and Optimization of Novel SaFabI Inhibitors as Specific Therapeutic Agents for MRSA Infection.
J Med Chem 67: 10096-10134
Sichuan University
Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.
J Med Chem 67: 10490-10507
Seoul National University
Design and synthesis of novel fluorene derivatives as inhibitors of pyruvate dehydrogenase kinase.
Bioorg Med Chem Lett 109:
Japan Tobacco
Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity.
J Med Chem 67: 10012-10024
Tampere University
Derivatives of D(-) glutamine-based MMP-2 inhibitors as an effective remedy for the management of chronic myeloid leukemia-Part-I: Synthesis, biological screening and in silico binding interaction analysis.
Eur J Med Chem 274:
Jadavpur University
Discovery of a potent and selective JAK1-targeting PROTAC degrader with anti-tumor activities.
Bioorg Med Chem Lett 109:
Shenyang Pharmaceutical University
Design, synthesis and antiproliferative activity of raloxifene/histone deacetylase inhibitor hybrids in breast cancer.
Eur J Med Chem 274:
McGill University
Research progress on GPX4 targeted compounds.
Eur J Med Chem 274:
Peking University
Poly (ADP-ribose) polymerase (PARP) inhibitors as anticancer agents: An outlook on clinical progress, synthetic strategies, biological activity, and structure-activity relationship.
Eur J Med Chem 274:
Acharya & BM Reddy College of Pharmacy
Discovery of novel benzimidazole derivatives as selective and reversible monoamine oxidase B inhibitors for Parkinson's disease treatment.
Eur J Med Chem 274:
Zhejiang University
Overcoming Secondary Mutations of Type II Kinase Inhibitors.
J Med Chem 67: 9776-9788
University of Arkansas
A consensus reverse docking approach for identification of a competitive inhibitor of acetyltransferase enhanced intracellular survival protein from Mycobacterium tuberculosis.
Bioorg Med Chem 108:
Federal University of Sergipe
The recent discovery of a promising pharmacological scaffold derived from carvacrol: A review.
Bioorg Med Chem Lett 109:
Universiti Kebangsaan Malaysia
Discovery and Optimization of Tetrahydroisoquinoline Derivatives To Enhance Lysosome Biogenesis as Preclinical Candidates for the Treatment of Alzheimer's Disease.
J Med Chem 67: 8836-8861
Nanjing University of Chinese Medicine
Discovery of a Promising CBP/p300 Degrader XYD129 for the Treatment of Acute Myeloid Leukemia.
J Med Chem 67: 9194-9213
Shenyang Pharmaceutical University
Synthesis and evaluation of 3-hydroxyquinolin-2(1H)-one derivatives as inhibitors of tyrosinase.
Bioorg Med Chem Lett 109:
North-West University
Dual-target inhibitors of colchicine binding site for cancer treatment.
Eur J Med Chem 274:
Henan University
Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors.
Eur J Med Chem 274:
Fudan University
Structure-based design of multitargeting ChEs-MAO B inhibitors based on phenyl ring bioisosteres: AChE/BChE selectivity switch and drug-like characterization.
Eur J Med Chem 274:
University of Bari Aldo Moro
Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA.
J Med Chem 67: 9759-9771
Pfizer
Structure-Based Design and Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High Selectivity, Brain Penetration, and In Vivo Efficacy.
J Med Chem 67: 9431-9446
Suzhou Genhouse Bio
X-ray Structure-Guided Discovery of a Potent Benzimidazole Glutaminyl Cyclase Inhibitor That Shows Activity in a Parkinson's Disease Mouse Model.
J Med Chem 67: 8730-8756
Sichuan University
Identification of highly potent and selective HTRA1 inhibitors.
Bioorg Med Chem Lett 109:
Stanford University
Design, Synthesis, and Structure-Activity Relationships of Novel Peptide Derivatives of the Severe Acute Respiratory Syndrome-Coronavirus-2 Spike-Protein that Potently Inhibit Nicotinic Acetylcholine Receptors.
J Med Chem 67: 9587-9598
University of Utah
Systematic Structure-Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments.
J Med Chem 67: 9552-9574
Virginia Commonwealth University
A new framework for novel analogues of pazopanib as potent and selective human carbonic anhydrase inhibitors: Design, repurposing rational, synthesis, crystallographic, in vivo and in vitro biological assessments.
Eur J Med Chem 274:
Tanta University
Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.
J Med Chem 67: 9173-9193
University of Kentucky
Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer.
J Med Chem 67: 8913-8931
Zhongnan Hospital of Wuhan University
Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.
J Med Chem 67: 8585-8608
Genentech
Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure.
J Med Chem 67: 9731-9744
Bristol Myers Squibb
Small molecules that regulate the N6-methyladenosine RNA modification as potential anti-cancer agents.
Eur J Med Chem 274:
University of Connecticut
Recent advances in targeting histone H3 lysine 36 methyltransferases for cancer therapy.
Eur J Med Chem 274:
China Pharmaceutical University
Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders.
J Med Chem 67: 9355-9373
Intra-Cellular Therapies, Inc.
Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.
J Med Chem 67: 8545-8568
Galapagos NV
Discovery of the Selective and Orally Available Galectin-1 Inhibitor GB1908 as a Potential Treatment for Lung Cancer.
J Med Chem 67: 9374-9388
Galecto Biotech AB
Amide bioisosteric replacement in the design and synthesis of quorum sensing modulators.
Eur J Med Chem 273:
Hubei University of Education
SETDB1 as a cancer target: challenges and perspectives in drug design.
RSC Med Chem 15: 1424-1451
University of Sao Paulo
Hijacking monopolar spindle 1 (MPS1) for various cancer types by small molecular inhibitors: Deep insights from a decade of research and patents.
Eur J Med Chem 273:
Shaanxi University of Science & Technology
Exploring fluorine-substituted piperidines as potential therapeutics for diabetes mellitus and Alzheimer's diseases.
Eur J Med Chem 273:
University of Gujrat
Comprehensive analysis of resorcinyl-imidazole Hsp90 inhibitor design.
Eur J Med Chem 273:
Vilnius University
Application and challenges of nitrogen heterocycles in PROTAC linker.
Eur J Med Chem 273:
University of South China
Discovery of 3-((4-Benzylpyridin-2-yl)amino)benzamides as Potent GPR52 G Protein-Biased Agonists.
J Med Chem 67: 9709-9730
University of Texas Medical Branch
Design, Synthesis, and Biological Evaluation of New 2,6,7-Substituted Purine Derivatives as Toll-like Receptor 7 Agonists for Intranasal Vaccine Adjuvants.
J Med Chem 67: 9389-9405
Gwangju Institute of Science and Technology
Structure-Based Design of a Potent and Selective YTHDC1 Ligand.
J Med Chem 67: 9516-9535
University of Zurich
Computational design, synthesis, and assessment of 3-(4-(4-(1,3,4-oxadiazol-2-yl)-1H-imidazol-2-yl)phenyl)-1,2,4-oxadiazole derivatives as effective epidermal growth factor receptor inhibitors: a prospective strategy for anticancer therapy.
RSC Med Chem 15: 1626-1639
Lupin Ltd.
Coumarin-furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies.
RSC Med Chem 15: 1565-1577
Hubei University
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes.
RSC Med Chem 15: 1773-1781
University of Cambridge
Imidazopyrimidine: from a relatively exotic scaffold to an evolving structural motif in drug discovery.
RSC Med Chem 15: 1488-1507
National Institute of Pharmaceutical Education and Research Ahmedabad (NIPER-A)
Helical sulfonyl-γ-AApeptides for the inhibition of HIV-1 fusion and HIF-1α signaling.
RSC Med Chem 15: 1418-1423
University of South Florida
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections.
RSC Med Chem 15: 1589-1600
Universite degli Studi di Parma Viale delle Scienze
PDE-stable 2'3'-cGAMP analogues, containing 5'-S-phosphorothioester linkage, as STING agonists.
RSC Med Chem 15: 1508-1514
Purdue University
Substituted 4-methylcoumarin inhibitors of SLC26A3 (DRA) for treatment of constipation and hyperoxaluria.
RSC Med Chem 15: 1731-1736
San Francisco State University
Carltonine-derived compounds for targeted butyrylcholinesterase inhibition.
RSC Med Chem 15: 1601-1625
Charles University
A colorimetric assay adapted to fragment screening revealing aurones and chalcones as new arginase inhibitors.
RSC Med Chem 15: 1722-1730
Universite de Franche-Comte
Pyrazolopyridine-based kinase inhibitors for anti-cancer targeted therapy.
RSC Med Chem 15: 1452-1470
Indian Institute of Technology
In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel.
J Med Chem 67: 9124-9149
University of Messina
Replacement of the hydroxamic acid group in the selective HDAC8 inhibitor PCI-34051.
Bioorg Med Chem Lett 108:
University of Pittsburgh
The role of the methoxy group in approved drugs.
Eur J Med Chem 273:
Takeda Pharmaceuticals
Metabolomic Analysis and Antiviral Screening of a Marine Algae Library Yield Jobosic Acid (2,5-Dimethyltetradecanoic Acid) as a Selective Inhibitor of SARS-CoV-2.
J Nat Prod 87: 1513-1520
University of Puerto Rico-Medical Sciences Campus
Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
J Med Chem 67: 8609-8629
Universidade Estadual de Campinas
Discovery of novel small molecules targeting the USP21/JAK2/STAT3 axis for the treatment of triple-negative breast cancer.
Eur J Med Chem 273:
University of South China
Leveraging a rationally designed veliparib-based anilide eliciting anti-leukemic effects for the design of pH-responsive polymer nanoformulation.
Eur J Med Chem 273:
Taipei Medical University
Discovery of first-in-class highly selective TRPV1 antagonists with dual analgesic and hypoglycemic effects.
Bioorg Med Chem 107:
The First Affiliated Hospital of Zhengzhou University
Development of Penicillin-Based Carbonic Anhydrase Inhibitors Targeting Multidrug-Resistant Neisseria gonorrhoeae.
J Med Chem 67: 9613-9627
University of Florence
Design of Selective PARP-1 Inhibitors and Antitumor Studies.
J Med Chem 67: 8877-8901
Shandong University
Novel 4-triazole phenyl amide (4-TPA) molecules: Potent promoters of α-synuclein fibril disassembly.
Eur J Med Chem 273:
Fudan University
Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
J Med Chem 67: 8988-9027
AstraZeneca
Development of Novel Phosphonodifluoromethyl-Containing Phosphotyrosine Mimetics and a First-In-Class, Potent, Selective, and Bioavailable Inhibitor of Human CDC14 Phosphatases.
J Med Chem 67: 8817-8835
Purdue University
Structure-Based Optimization of Novel Sterol 24-C-Methyltransferase Inhibitors for the Treatment of Candida albicans Infections.
J Med Chem 67: 9318-9341
Shandong University
Design, synthesis, molecular modeling, in vitro and in vivo biological evaluation of potent anthranilamide derivatives as dual P-glycoprotein and CYP3A4 inhibitors.
Eur J Med Chem 273:
University of Nebraska Medical Center
Discovery of meisoindigo derivatives as noncovalent and orally available Mpro inhibitors: their therapeutic implications in the treatment of COVID-19.
Eur J Med Chem 273:
Central South University
Pyrrole-containing hybrids as potential anticancer agents: An insight into current developments and structure-activity relationships.
Eur J Med Chem 273:
Jiangxi Science & Technology Normal University
Piezo1 and its inhibitors: Overview and perspectives.
Eur J Med Chem 273:
Hanoi University of Pharmacy
An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy.
Eur J Med Chem 272:
University of Chinese Academy of Sciences
Design and synthesis of novel thiazole-derivatives as potent ALK5 inhibitors.
Bioorg Med Chem Lett 108:
Carna Biosciences, Inc.
Design, synthesis and biological evaluation of 4-(indolin-1-yl)-6-substituted-pyrido[3,2-d]pyrimidine derivatives as Mnk1/2 inhibitors.
Eur J Med Chem 272:
Shenyang Pharmaceutical University
Current therapy in amyotrophic lateral sclerosis (ALS): A review on past and future therapeutic strategies.
Eur J Med Chem 272:
Nanjing University of Chinese Medicine
An Improved PDE6D Inhibitor Combines with Sildenafil To Inhibit KRAS Mutant Cancer Cell Growth.
J Med Chem 67: 8569-8584
University of Luxembourg
Discovery of DS44470011: An oral hypoxia-inducible factor prolyl hydroxylase inhibitor for the treatment of renal anemia.
Bioorg Med Chem Lett 108:
Daiichi Sankyo Co., Ltd.
α-Fluorination of tropane compounds and its impact on physicochemical and ADME properties.
Bioorg Med Chem Lett 108:
Eisai Co., Ltd.
Macrocyclization strategy for improving candidate profiles in medicinal chemistry.
Eur J Med Chem 272:
Gachon University
Discovery of Novel Azaindoles as Potent and Selective PI3Kδ Inhibitors for Treatment of Multiple Sclerosis.
J Med Chem 67: 9628-9644
Zhejiang University
WLB-87848, a Selective σ1 Receptor Agonist, with an Unusually Positioned NH Group as Positive Ionizable Moiety and Showing Neuroprotective Activity.
J Med Chem 67: 9150-9164
Welab Barcelona
Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs.
J Med Chem 67: 8757-8790
University of Bonn
Hit-to-Lead Optimization of the Natural Product Oridonin as Novel NLRP3 Inflammasome Inhibitors with Potent Anti-Inflammation Activity.
J Med Chem 67: 9406-9430
China Pharmaceutical University
Lead compound profiling for small molecule inhibitors of the REV1-CT/RIR Translesion synthesis Protein-Protein interaction.
Bioorg Med Chem 106:
University of Connecticut
Design, synthesis and evaluation of novel prostate-specific membrane antigen-targeted aryl [18F]fluorosulfate PET tracers.
Bioorg Med Chem 106:
Fudan University
Discovery of indole-2-one derivatives as BRD4 (BD1) selective inhibitors.
Bioorg Med Chem 106:
Lanzhou University
Discovery of an efficacious KDM5B PROTAC degrader GT-653 up-regulating IFN response genes in prostate cancer.
Eur J Med Chem 272:
East China Normal University
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.
J Med Chem 67: 9447-9464
Wenzhou Medical University Lishui Hospital
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
J Med Chem 67: 8708-8729
Genentech
Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation.
J Med Chem 67: 8642-8666
University of Florida
Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches.
J Med Chem 67: 8962-8987
AstraZeneca
A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors.
ACS Med Chem Lett 15: 714-721
Biogen
Novel CD73 Inhibitors for Treating Cancer.
ACS Med Chem Lett 15: 571-572
Smith, Gambrell & Russell
Pyrrolidinone Derivatives as NIK Inhibitors for Treating Autoimmune and Inflammatory Diseases.
ACS Med Chem Lett 15: 581-582
Smith, Gambrell & Russell
Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders.
ACS Med Chem Lett 15: 659-666
Sun Yat-sen University
Structural Investigations of Phthalazinone Derivatives as Allosteric Inhibitors of Human DNA Methyltransferase 3A.
ACS Med Chem Lett 15: 590-594
University of California
Synthesis and Monoamine Oxidase Inhibitory Activity of Halogenated Flavones.
ACS Med Chem Lett 15: 610-618
University of South Carolina
Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers.
ACS Med Chem Lett 15: 595-601
HUTCHMED Limited
Novel Myeloperoxidase Inhibitors for Treating Multiple Diseases.
ACS Med Chem Lett 15: 569-570
Smith, Gambrell & Russell
Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment.
ACS Med Chem Lett 15: 646-652
Cerevance Limited
Discovery of Novel Bicyclic Pyrazoles as Potent PIP5K1C Inhibitors.
ACS Med Chem Lett 15: 684-690
Kyorin Pharmaceutical Co., Ltd.
Identification of Selective Imidazopyridine CSF1R Inhibitors.
ACS Med Chem Lett 15: 722-730
Sanofi R&D
Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors.
Bioorg Med Chem 106:
University of Arkansas for Medical Sciences
Structure-Activity Relationships toward the Identification of a High-Potency Selective Human Toll-like Receptor-7 Agonist.
J Med Chem 67: 8346-8360
Panjab University
Discovery of Oral AMP-Activated Protein Kinase Activators for Treating Hyperlipidemia.
J Med Chem 67: 7870-7890
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy.
J Med Chem 67: 7995-8019
Southern Medical University
Inhibitory interactions of the 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one scaffold with Bunyavirales cap-snatching endonucleases expose relevant drug design features.
Eur J Med Chem 272:
University of Parma
Design, synthesis of ceramide 1-phosphate analogs and their affinity for cytosolic phospholipase A2 as evidenced by surface plasmon resonance.
Bioorg Med Chem Lett 107:
Research Foundation ITSUU Laboratory
Recent advances in c-Met-based dual inhibitors in the treatment of cancers.
Eur J Med Chem 272:
Liaoning University
Impact of Combinatorial Histone Modifications on Acetyllysine Recognition by the ATAD2 and ATAD2B Bromodomains.
J Med Chem 67: 8186-8200
University of Vermont
Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility.
J Med Chem 67: 7825-7835
Cytokinetics, Inc.
Analogues of the pan-selectin antagonist rivipansel (GMI-1070).
Eur J Med Chem 272:
University of Basel
Recent advances and future directions on small molecule VEGFR inhibitors in oncological conditions.
Eur J Med Chem 272:
Taipei Medical University
Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches.
J Med Chem 67: 8141-8160
Novartis
A β-Carboline Derivate PAD4 Inhibitor Reshapes Neutrophil Phenotype and Improves the Tumor Immune Microenvironment against Triple-Negative Breast Cancer.
J Med Chem 67: 7973-7994
Capital Medical University
Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases.
J Med Chem 67: 8077-8098
Idorsia Pharmaceuticals Ltd.
Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity.
J Med Chem 67: 8406-8419
Wuyi University
Design of FK866-Based Degraders for Blocking the Nonenzymatic Functions of Nicotinamide Phosphoribosyltransferase.
J Med Chem 67: 8099-8121
Beijing University of Chinese Medicine
Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases.
J Med Chem 67: 8060-8076
Hangzhou Medical College
Discovery of potent small molecule ubiquitin-specific protease 10 inhibitors with anti-hepatocellular carcinoma activity through regulating YAP expression.
Eur J Med Chem 272:
Zhejiang University
Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor.
Eur J Med Chem 272:
East China Normal University
Design, synthesis, and biological evaluation of novel sesquiterpene lactone derivatives as PKM2 activators with potent anti-ulcerative colitis activities.
Eur J Med Chem 272:
Nanjing University of Chinese Medicine
Exploring the Structural Attributes of Yoda1 for the Development of New-Generation Piezo1 Agonist Yaddle1 as a Vaccine Adjuvant Targeting Optimal T Cell Activation.
J Med Chem 67: 8225-8246
CSIR-Indian Institute of Chemical Biology
Selenization of Small Molecule Drugs: A New Player on the Board.
J Med Chem 67: 7759-7787
University of Navarra
Discovery of Glutamate Carboxypeptidase III Ligands to Compete the Uptake of [177Lu]Lu-PSMA-617 in Healthy Organs.
J Med Chem 67: 8247-8260
Philochem
Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor.
Bioorg Med Chem Lett 107:
Nanjing University of Chinese Medicine
Preferential HDAC6 inhibitors derived from HPOB exhibit synergistic antileukemia activity in combination with decitabine.
Eur J Med Chem 272:
Leipzig University
Recent discovery and development of AXL inhibitors as antitumor agents.
Eur J Med Chem 272:
Sichuan University
A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo.
J Med Chem 67: 7921-7934
Xiamen University
Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell.
J Med Chem 67: 7935-7953
Leiden University
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
J Med Chem 67: 8122-8140
Biogen Research and Development
Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update.
J Med Chem 67: 7668-7758
Eberhard Karls University Tubingen
Direct Inhibition of BK Channels by Cannabidiol, One of the Principal Therapeutic Cannabinoids Derived from Cannabis sativa.
J Nat Prod 87: 1368-1375
Universidad Nacional de La Plata - CICPBA - CONICET
Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma.
J Med Chem 67: 8445-8459
Sungkyunkwan University
Modulation of proteasome subunit selectivity of syringolins.
Bioorg Med Chem 106:
Hokkaido University
Discovery of 4-benzylpiperazinequinoline BChE inhibitor that suppresses neuroinflammation for the treatment of Alzheimer's disease.
Eur J Med Chem 272:
China Pharmaceutical University
Synthesis and Evaluation of diaryl ether modulators of the leukotriene A4 hydrolase aminopeptidase activity.
Eur J Med Chem 272:
George Mason University
Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM).
Eur J Med Chem 272:
First People's Hospital of Shangqiu
Exploration of novel isoxazole-fused quinone derivatives as anti-colorectal cancer agents through inhibiting STAT3 and elevating ROS level.
Eur J Med Chem 272:
Sichuan University
From lab to nature: Recent advancements in the journey of gastroprotective agents from medicinal chemistry to phytotherapy.
Eur J Med Chem 272:
Birla Institute of Technology
Lead optimization based design, synthesis, and pharmacological evaluation of quinazoline derivatives as multi-targeting agents for Alzheimer's disease treatment.
Eur J Med Chem 271:
Indian Institute of Technology-Banaras Hindu University
Perspectives and challenges in developing small molecules targeting purine nucleoside phosphorylase.
Eur J Med Chem 271:
Sichuan University
Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application.
J Med Chem 67: 7788-7824
China Pharmaceutical University
Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1.
J Med Chem 67: 8172-8185
University of California Riverside
Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation.
J Med Chem 67: 8383-8395
Biogen Inc.
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.
J Med Chem 67: 7836-7858
BeiGene(Beiing) Co., Ltd.
Design, synthesis and structure-activity relationship of 1,8-naphthalimide derivatives as highly potent hCYP1B1 inhibitors.
Bioorg Med Chem Lett 107:
Nanjing University of Chinese Medicine
Total synthesis/semi-synthesis of natural isopentenyl flavonoids with inhibitory activity on NLRP3 inflammasome.
Bioorg Med Chem Lett 107:
East China University of Science and Technology
Targeting the cysteine biosynthesis pathway in microorganisms: Mechanism, structure, and drug discovery.
Eur J Med Chem 271:
Southwest University
Discovery of potent and novel dual NAMPT/BRD4 inhibitors for efficient treatment of hepatocellular carcinoma.
Eur J Med Chem 271:
Xinxiang Medical University
Design, synthesis, and biological evaluation of 5-(1H-indol-5-yl)isoxazole-3-carboxylic acids as novel xanthine oxidase inhibitors.
Eur J Med Chem 271:
Wuhan Institute of Technology
Structure-activity relationship in NOD2 agonistic muramyl dipeptides.
Eur J Med Chem 271:
Panjab University
Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain.
J Med Chem 67: 11662-11687
Universite Paris Cite
Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer.
J Med Chem 67: 8161-8171
Insilico Medicine Shanghai Ltd
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis.
Eur J Med Chem 271:
Anhui Medical University
A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
J Med Chem 67: 13550-13571
Pfizer
Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase.
J Med Chem 67: 7385-7405
Soochow University
Illuminating Dark Chemical Matter Using the Cell Painting Assay.
J Med Chem 67: 8862-8876
Max-Planck Institute Institute of Molecular Physiology
Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader.
J Med Chem 67: 6938-6951
Shanghai Institute of Organic Chemistry
Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects.
J Med Chem 67: 7603-7619
Vrije Universiteit Brussel
Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.
J Med Chem 67: 7516-7538
Sichuan University
Medicinal chemistry strategies toward broad-spectrum antiviral agents to prevent next pandemics.
Eur J Med Chem 271:
State Key Laboratory of NBC Protection for Civilian
Concurrent Optimizations of Efficacy and Blood-Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson's Disease Therapeutics.
J Med Chem 67: 7647-7662
Korea Advanced Institute of Science and Technology (KAIST)
Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells.
J Med Chem 67: 7176-7196
Shanghai Jiao Tong University
Improving tumor sensitivity by the introduction of an ester chain to triaryl derivatives targeting PD-1/PD-L1.
Eur J Med Chem 271:
China Pharmaceutical University
High affinity and low PARP-trapping benzimidazole derivatives as a potential warhead for PARP1 degraders.
Eur J Med Chem 271:
University of South China
Synthesis of a new 2-prenylated quinoline as potential drug for metabolic syndrome with pan-PPAR activity and anti-inflammatory effects.
Bioorg Med Chem Lett 106:
University of Valencia
Discovery of the small molecular inhibitors against sclerostin loop3 as potential anti-osteoporosis agents by structural based virtual screening and molecular design.
Eur J Med Chem 271:
Hong Kong Baptist University
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation.
J Med Chem 67: 7283-7300
China Pharmaceutical University
Development of Benziodarone Analogues with Enhanced Potency for Selective Binding to Transthyretin in Human Plasma.
J Med Chem 67: 6987-7005
University of Toyama
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.
Bioorg Med Chem Lett 107:
WuXi AppTec
Quinazolines annelated at the N(3)-C(4) bond: Synthesis and biological activity.
Eur J Med Chem 271:
Ural Federal University
Tetrahydropyridine LIMK inhibitors: Structure activity studies and biological characterization.
Eur J Med Chem 271:
University of Orleans
1,2,3-Triazole-totarol conjugates as potent PIP5K1α lipid kinase inhibitors.
Bioorg Med Chem 105:
Universitat Munster
Design, Synthesis, and Evaluation of Dihydropyrimidine Derivatives as Selective PDE1 Inhibitors for the Treatment of Liver Fibrosis.
J Med Chem 67: 8309-8322
Hainan University
Discovery of novel SOS1 inhibitors using machine learning.
RSC Med Chem 15: 1392-1403 (2024)
University of Nottingham Ningbo China
Small molecules modulating RNA splicing: a review of targets and future perspectives.
RSC Med Chem 15: 1109-1126 (2024)
University of Bordeaux
A novel BODIPY-based theranostic agent for
RSC Med Chem 15: 1216-1224 (2024)
Shanghai Institute of Materia Medica
Progress in small-molecule inhibitors targeting PD-L1.
RSC Med Chem 15: 1161-1175 (2024)
Henan University
Design, synthesis,
RSC Med Chem 15: 1329-1347 (2024)
Central University of Punjab
Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity.
RSC Med Chem 15: 1247-1257 (2024)
University of Florence
1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists.
RSC Med Chem 15: 1210-1215 (2024)
University of Groningen
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water.
RSC Med Chem 15: 1274-1282 (2024)
Kindai University
Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1.
RSC Med Chem 15: 1096-1108 (2024)
China Pharmaceutical University
Screening of efficient salicylaldoxime reactivators for DFP and paraoxon-inhibited acetylcholinesterase.
RSC Med Chem 15: 1225-1235 (2024)
Air Force Medical University
Design, synthesis, and biological evaluation of some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide hybrids as MTDLs for Alzheimer's disease therapy.
Eur J Med Chem 271:
Indian Institute of Technology - Banaras Hindu University
Design, synthesis, and biological evaluation of 3-phenyl substituted pyridine derivatives as potential dual inhibitors of XOR and URAT1.
Eur J Med Chem 271:
South China University of Technology
Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer.
J Med Chem 67: 7330-7358
Guizhou Medical University
Identification of naphthalimide-derivatives as novel PBD-targeted polo-like kinase 1 inhibitors with efficacy in drug-resistant lung cancer cells.
Eur J Med Chem 271:
Guangxi Normal University
Druglike, 18F-labeled PET Tracers Targeting Fibroblast Activation Protein.
J Med Chem 67: 7068-7087
University of Antwerp
Benzothiazole derivatives as histone deacetylase inhibitors for the treatment of autosomal dominant polycystic kidney disease.
Eur J Med Chem 271:
Xuzhou Medical University
Probing benzenesulfonamide-thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase II.
Eur J Med Chem 271:
Cairo University
Development of Prolinol Containing Inhibitors of Hypoxanthine-Guanine-Xanthine Phosphoribosyltransferase: Rational Structure-Based Drug Design.
J Med Chem 67: 7158-7175
The University of Queensland
Discovery of Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation.
J Med Chem 67: 8667-8692
China Pharmaceutical University
Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound.
J Med Chem 67: 7260-7275
Hangzhou Normal University
Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity.
J Med Chem 67: 6952-6986
Guangzhou Institutes of Biomedicine and Health
Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists.
J Med Chem 67: 7224-7244
University of Copenhagen
Psychoplastogenic DYRK1A Inhibitors with Therapeutic Effects Relevant to Alzheimer's Disease.
J Med Chem 67: 6922-6937
University of California
Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect.
J Med Chem 67: 7112-7129
Fudan University
Discovery of N-(4-((6-(3,5- Dimethoxyphenyl)-9H-purine derivatives as irreversible covalent FGFR inhibitors.
Eur J Med Chem 271:
Southeast University
Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles.
J Med Chem 67: 7406-7430
Tanta University
Biological evaluation of sulfonate and sulfate analogues of lithocholic acid: A bioisosterism-guided approach towards the discovery of potential sialyltransferase inhibitors for antimetastatic study.
Bioorg Med Chem Lett 105:
National Yang Ming Chiao Tung University
Discovery of novel pyridone-benzamide derivatives possessing a 1-methyl-2-benzimidazolinone moiety as potent EZH2 inhibitors for the treatment of B-cell lymphomas.
Bioorg Med Chem 105:
Shenyang Pharmaceutical University
Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease.
J Med Chem 67: 7146-7157
Florida International University
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.
Eur J Med Chem 271:
University of North Carolina at Chapel Hill
Development of benzimidazole-based compounds as novel capsid assembly modulators for the treatment of HBV infection.
Eur J Med Chem 271:
Ocean University of China
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
J Med Chem 67: 7245-7259
University of Oxford
Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors.
J Med Chem 67: 7620-7634
Central South University
In vitro inhibition of α-Synuclein aggregation and disaggregation of preformed fibers by polyphenol hybrids with 2-conjugated benzothiazole.
Bioorg Med Chem Lett 105:
Zhengzhou University
Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents.
J Med Chem 67: 7585-7602
Wenzhou Medical University
Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors.
J Med Chem 67: 7048-7067
Center for Free-Electron Laser Science CFEL
Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer.
J Med Chem 67: 7130-7145
China Pharmaceutical University
Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist.
ACS Med Chem Lett 15: 478-485 (2024)
Crinetics Pharmaceuticals
In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
ACS Med Chem Lett 15: 540-545 (2024)
Pfizer
Novel Isoxazolidines as RIPK1 Inhibitors for Treating Alzheimer's Disease, Multiple Sclerosis, and Amyotrophic Lateral Sclerosis.
ACS Med Chem Lett 15: 447-448 (2024)
Smith, Gambrell & Russell
Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions.
ACS Med Chem Lett 15: 486-492 (2024)
Janssen Research and Development
Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.
ACS Med Chem Lett 15: 533-539 (2024)
Whitman College
Design, Synthesis, and Evaluation of 8-(
ACS Med Chem Lett 15: 518-523 (2024)
Huaqiao University
The Science and Art of Structure-Based Virtual Screening.
ACS Med Chem Lett 15: 436-440 (2024)
Astrazeneca
Novel ACC Inhibitors for Treating Acne.
ACS Med Chem Lett 15: 445-446 (2024)
Smith, Gambrell & Russell
Imidazole Bioisostere Activators of Endopeptidase Neurolysin with Enhanced Potency and Metabolic Stability.
ACS Med Chem Lett 15: 510-517 (2024)
University of Nebraska Medical Center
Novel Phosphorylpurinone Compounds for Treating Cancer.
ACS Med Chem Lett 15: 441-442 (2024)
Smith, Gambrell & Russell
Discovery of a New Class of 1-(4-Sulfamoylbenzoyl)piperidine-4-carboxamides as Human Carbonic Anhydrase Inhibitors.
ACS Med Chem Lett 15: 470-477 (2024)
University of Cagliari
Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.
ACS Med Chem Lett 15: 501-509 (2024)
University of Nottingham
Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable
ACS Med Chem Lett 15: 524-532 (2024)
Sanders Tri-Institutional Therapeutics
Novel PCSK9 Inhibitors for Treating Cardiovascular Diseases.
ACS Med Chem Lett 15: 443-444 (2024)
Smith, Gambrell & Russell
Synthesis and Structure-Activity Relationships for Glutamate Transporter Allosteric Modulators.
J Med Chem 67: 6119-6143
Drexel University College of Medicine
Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer.
Eur J Med Chem 271:
Yantai University
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor.
Eur J Med Chem 271:
Nankai University
Exploration of isoxazole analogs: Synthesis, COX inhibition, anticancer screening, 3D multicellular tumor spheroids, and molecular modeling.
Eur J Med Chem 271:
An-Najah National University
Modulators for palmitoylation of proteins and small molecules.
Eur J Med Chem 271:
Hebei University
Expanding the ligand spaces for E3 ligases for the design of protein degraders.
Bioorg Med Chem 105:
Goethe-University Frankfurt
Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity.
J Med Chem 67: 6769-6792
Sichuan University
Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3'-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury.
J Med Chem 67: 6268-6291
Shanghai Jiao Tong University
Discovery of novel amide derivatives as potent quorum sensing inhibitors of Pseudomonas aeruginosa.
Eur J Med Chem 271:
South China Agricultural University
Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases.
Eur J Med Chem 271:
Qingdao University
Tetrazole derivatives in the management of neurological disorders: Recent advances on synthesis and pharmacological aspects.
Eur J Med Chem 271:
Banasthali Vidyapith
Discovery of Novel Aryl Triazolone Dihydropyridines (ATDPs) Targeting Highly Conserved Residue W229 as Promising HIV-1 NNRTIs.
J Med Chem 67: 6570-6584
Shandong University
Structure-Guided Discovery and Preclinical Assessment of Novel (Thiophen-3-yl)aminopyrimidine Derivatives as Potent ERK1/2 Inhibitors.
J Med Chem 67: 6425-6455
Sichuan University
Discovery andsynthesis of novel benzoylhydrazone neuraminidase inhibitors.
Bioorg Med Chem Lett 105:
Shanghai Institute of Technology
Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.
J Med Chem 67: 6495-6507
Texas A&M University
Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader.
J Med Chem 67: 6880-6892
Icahn School of Medicine At Mount Sinai
Discovery of novel nucleoside derivatives as selective lysine acetyltransferase p300 inhibitors for cancer therapy.
Bioorg Med Chem Lett 104:
Changsha Medical University
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles.
J Med Chem 67: 6549-6569
Eberhard Karls University Tubingen
Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors.
Eur J Med Chem 270:
Insilico Medicine Shanghai Ltd
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors.
Eur J Med Chem 270:
Nerviano Medical Sciences S.r.l.
Structural modification of tanshinone IIA and their α-glucosidase inhibitory activity.
Bioorg Med Chem Lett 105:
Chulalongkorn University
The mechanism of covalent inhibition of LAR phosphatase by illudalic acid.
Bioorg Med Chem Lett 104:
University of Utah
Potentiating Activity of GmhA Inhibitors on Gram-Negative Bacteria.
J Med Chem 67: 6610-6623
Mutabilis
Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.
J Med Chem 67: 5963-5998
Shenyang Pharmaceutical University
Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers.
J Med Chem 67: 6064-6080
Tango Therapeutics
Active site-directed probes targeting dipeptidyl peptidases 8 and 9.
Eur J Med Chem 270:
University of Antwerp
Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist.
J Med Chem 67: 6144-6188
Cybin IRL
Discovery of a Novel CSF-1R Inhibitor with Highly Improved Pharmacokinetic Profiles and Superior Efficacy in Colorectal Cancer Immunotherapy.
J Med Chem 67: 6854-6879
Nanjing University of Chinese Medicine
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises.
J Med Chem 67: 6052-6063
TU Dortmund University and Drug Discovery Hub Dortmund (DDHD)
Discovery of 2-Amide-3-methylester Thiophenes that Target SARS-CoV-2 Mac1 and Repress Coronavirus Replication, Validating Mac1 as an Antiviral Target.
J Med Chem 67: 6519-6536
University of Oulu
Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer.
Eur J Med Chem 270:
China Pharmaceutical University
Advances in TRPV6 inhibitors for tumors by targeted therapies: Macromolecular proteins, synthetic small molecule compounds, and natural compounds.
Eur J Med Chem 270:
Hunan Normal University
Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy.
J Med Chem 67: 6253-6267
The Sixth Affiliated Hospital of Wenzhou Medical University
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.
J Med Chem 67: 6099-6118
Tianjin University
Discovery of novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 2 inhibitors.
Bioorg Med Chem 104:
Tianjin University
Antascomicin B stabilizes FKBP51-Akt1 complexes as a molecular glue.
Bioorg Med Chem Lett 104:
Technical University Darmstadt
Histone deacetylase (HDAC) inhibitor specificity determinants are preserved in a class of dual HDAC/non-covalent proteasome inhibitors.
Bioorg Med Chem 104:
University of Maryland
Discovery of ganoderic acid A (GAA) PROTACs as MDM2 protein degraders for the treatment of breast cancer.
Eur J Med Chem 270:
Chinese Academy of Medical Sciences and Peking Union Medical College
Synthesis and biological evaluation of 4-imidazolidinone-containing compounds as potent inhibitors of the MDM2/p53 interaction.
Eur J Med Chem 270:
Nanjing University of Chinese Medicine
Channeling Nicotinamide Phosphoribosyltransferase (NAMPT) to Address Life and Death.
J Med Chem 67: 5999-6026
University of Arizona
Design, synthesis and activity evaluation of quinolinone derivatives as EZH2 inhibitors.
Bioorg Med Chem Lett 105:
Southeast University
Novel 6-alkyl-bridged 4-arylalkylpiperazin-1-yl derivatives of azepino[4,3-b]indol-1(2H)-one as potent BChE-selective inhibitors showing protective effects against neurodegenerative insults.
Eur J Med Chem 270:
University of Bari Aldo Moro
Structure-based discovery of small molecule inhibitors of FKBP51-Hsp90 protein-protein interaction.
Eur J Med Chem 270:
Karolinska Institutet
Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements.
Bioorg Med Chem 104:
UCB
Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia.
J Med Chem 67: 6638-6657
Zhejiang University
Design, synthesis, and biological evaluation of first-in-class FABP1 inhibitors for the treatment of NASH.
Eur J Med Chem 270:
Guangdong Pharmaceutical University
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.
J Med Chem 67: 6313-6326
Zhejiang Sci-Tech University
Discovery of Highly Potent Solute Carrier 13 Member 5 (SLC13A5) Inhibitors for the Treatment of Hyperlipidemia.
J Med Chem 67: 6687-6704
China Pharmaceutical University
Drug development and potential targets for Cushing's syndrome.
Eur J Med Chem 270:
China Pharmaceutical University
Peptide Inhibitor Targeting the Extraterminal Domain in BRD4 Potently Suppresses Breast Cancer Both In Vitro and In Vivo.
J Med Chem 67: 6658-6672
Xiamen University
Targeting EGFR degradation by autophagosome degraders.
Eur J Med Chem 270:
Jinan University
Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma.
J Med Chem 67: 5437-5457
China Pharmaceutical University
Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications.
J Med Chem 67: 5185-5215
Sichuan University
Design, Synthesis, and Biological Evaluation of a Novel NIK Inhibitor with Anti-Inflammatory and Hepatoprotective Effects for Sepsis Treatment.
J Med Chem 67: 5617-5641
China Pharmaceutical University
Facile Synthesis and First Antifungal Exploration of Tetracyclic Meroterpenoids: (+)-Aureol, (-)-Pelorol, and Its Analogs.
J Nat Prod 87: 1092-1102 (2024)
Guizhou University
Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors.
J Med Chem 67: 5866-5882
University of North Carolina
Total Synthesis, Structure Reassignment, and Biological Evaluation of the Anti-Inflammatory Macrolactone 13-Hydroxy-14-deoxyoxacyclododecindione.
J Nat Prod 87: 1131-1149 (2024)
Johannes Gutenberg-University
Design, synthesis and biological evaluation of tanshinone IIA derivatives as NLRP3 inflammasome inhibitors.
Bioorg Med Chem Lett 104:
Guangzhou Medical University
Design, synthesis and biological evaluation of matrine contains benzimidazole derivatives as dual TOPOI and PARP inhibitors for cancer therapy.
Eur J Med Chem 270:
Guangxi University
Design, synthesis, and biological evaluation of aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.
Bioorg Med Chem 104:
Shanghai Institute of Pharmaceutical Industry Co., Ltd.
Discovery and characterization of potent spiro-isoxazole-based cereblon ligands with a novel binding mode.
Eur J Med Chem 270:
Saint Petersburg State University
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
J Med Chem 67: 5233-5258 (2024)
Galapagos
Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.
Eur J Med Chem 269:
Peking University
Discovery of pyrido[3,2-d]pyrimidin-6(5H)-one derivatives as checkpoint kinase 1 (CHK1) inhibitors with potent antitumor efficacy.
Eur J Med Chem 269:
Nanjing University of Chinese Medicine
Proline-derived quinoline formamide compounds as human urate transporter 1 inhibitors with potent uric acid-lowering activities.
Eur J Med Chem 269:
Peking Union Medical College
Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease.
J Med Chem 67: 5642-5661
Nanjing University of Chinese Medicine
5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein-Protein Interaction-Derived Functions.
J Med Chem 67: 5421-5436
University of Helsinki
Butyrylcholinesterase-Activated Near-Infrared Fluorogenic Probe for In Vivo Theranostics of Alzheimer's Disease.
J Med Chem 67: 6793-6809
China Pharmaceutical University
Model of P-Glycoprotein Ligand Binding and Validation with Efflux Substrate Matched Pairs.
J Med Chem 67: 5854-5865 (2024)
University of California
Synthesis, kinase inhibition and anti-leukemic activities of diversely substituted indolopyrazolocarbazoles.
Eur J Med Chem 269:
University Clermont Auvergne
Transient Receptor Potential Melastatin 7 (TRPM7) Ion Channel Inhibitors: Preliminary SAR and Conformational Studies of Xenicane Diterpenoids from the Hawaiian Soft Coral
J Nat Prod 87: 783-797 (2024)
Huazhong University of Science and Technology
Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.
J Med Chem 67: 5837-5853
Icahn School of Medicine At Mount Sinai
Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer.
J Med Chem 67: 5351-5372
University of Michigan
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
J Med Chem 67: 5259-5271
Pharmaron UK Ltd.
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
J Med Chem 67: 5216-5232 (2024)
Galapagos
Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy.
J Med Chem 67: 5783-5799
Tongji University
Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins.
J Med Chem 67: 5144-5167
Sichuan University
Improved synthesis, molecular modeling and anti-inflammatory activity of new fluorinated dihydrofurano-naphthoquinone compounds.
Bioorg Med Chem Lett 104:
Vietnam Academy of Science and Technology (VAST)
Guanidine-to-piperidine switch affords high affinity small molecule NPFF ligands with preference for NPFF1-R and NPFF2-R subtypes.
Eur J Med Chem 269:
University of Florida
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis.
Eur J Med Chem 269:
China Pharmaceutical University
A PSMA-targeted doxorubicin small-molecule drug conjugate.
Bioorg Med Chem Lett 104:
Washington State University
Targeting ATP-binding site of WRN Helicase: Identification of novel inhibitors through pocket analysis and Molecular Dynamics-Enhanced virtual screening.
Bioorg Med Chem Lett 104:
Sun Yat-sen University
Synergistic therapeutics: Co-targeting histone deacetylases and ribonucleotide reductase for enhanced cancer treatment.
Eur J Med Chem 269:
Manipal Academy of Higher Education
Exploiting high-energy hydration sites for the discovery of potent peptide aldehyde inhibitors of the SARS-CoV-2 main protease with cellular antiviral activity.
Bioorg Med Chem 103:
Takeda Development Center Americas, Inc
Fluorescent probes and degraders of the sterol transport protein Aster-A.
Bioorg Med Chem 103:
Technical University of Denmark
Discovery of novel polyheterocyclic neuraminidase inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone.
Eur J Med Chem 269:
Shanghai Institute of Technology
Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents.
Eur J Med Chem 269:
Shandong University
Discovery of Novel 5,6-Dihydro-4H-pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases.
J Med Chem 67: 5662-5682
Beijing University of Technology
Discovery of Novel 11-Membered Templates as Squalene Synthase Inhibitors.
J Med Chem 67: 5305-5314
Daiichi Sankyo RD Novare Co., Ltd.
Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy.
RSC Med Chem 15: 981-997 (2024)
Ain-Shams University
Deconvoluting low yield from weak potency in direct-to-biology workflows with machine learning.
RSC Med Chem 15: 1015-1021 (2024)
University of Cambridge
Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases.
RSC Med Chem 15: 963-980 (2024)
University of Rouen Normandy
Synthesis and bioactivity of psilocybin analogues containing a stable carbon-phosphorus bond.
RSC Med Chem 15: 998-1002 (2024)
Ghent University
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex.
RSC Med Chem 15: 1066-1071 (2024)
University of Toronto
-Arylsulfonamide-based adenosine analogues to target RNA cap
RSC Med Chem 15: 839-847 (2024)
University of Montpellier Cnrs
The medicinal chemistry evolution of antibody-drug conjugates.
RSC Med Chem 15: 809-831 (2024)
Abbvi
Reinvestigation of diphenylmethylpiperazine analogues of pyrazine as new class of
RSC Med Chem 15: 1022-1037 (2024)
Jamia Millia Islamia (A Central University)
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
RSC Med Chem 15: 856-873 (2024)
South China University
Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies.
RSC Med Chem 15: 788-808 (2024)
Tianjin University
Molecular editing of
RSC Med Chem 15: 937-962 (2024)
National Institute of Pharmaceutical Education and Research (NIPER)
Inhibition of N-type calcium channels by phenoxyaniline and sulfonamide analogues.
RSC Med Chem 15: 916-936 (2024)
Monash University
Recent advances in the exploration of oxazolidinone scaffolds from compound development to antibacterial agents and other bioactivities.
Eur J Med Chem 269:
Zhengzhou University
Discovery of DNL343: A Potent, Selective, and Brain-Penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases.
J Med Chem 67: 5758-5782
Denali Therapeutics Inc.
Long-Residence Time Peptide Antagonist for the Vasopressin V2 Receptor to Treat Autosomal Dominant Polycystic Kidney Disease.
J Med Chem 67: 5935-5944
Xuzhou Medical University
An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting M
Bioorg Med Chem Lett 103: (2024)
Ocean University of China
Evaluation of novel 2-(quinoline-2-ylthio)acetamide derivatives linked to diphenyl-imidazole as α-glucosidase inhibitors: Insights from in silico, in vitro, and in vivo studies on their anti-diabetic properties.
Eur J Med Chem 269:
Qom University of Technology
Progress on synthesis and structure-activity relationships of lamellarins over the past decade.
Eur J Med Chem 269:
Zhejiang Chinese Medical University
Synthesis and anti-liver fibrosis activity of imidazole and thiazole compounds containing amino acids.
Eur J Med Chem 269:
Yanbian University
Discovery of Alternative Binding Poses through Fragment-Based Identification of DHODH Inhibitors.
ACS Med Chem Lett 15: 381-387 (2024)
Janssen Pharmaceutical Research and Development
Pyrrolidinone Derivatives as NIK Inhibitors for Treating Inflammatory and Autoimmune Diseases.
ACS Med Chem Lett 15: 322-323 (2024)
Smith, Gambrell & Russell
Advancements in Predictive Medicine: NLRP3 Inflammasome Inhibitors and AI-Driven Predictive Health Analytics.
ACS Med Chem Lett 15: 331-333 (2024)
Usona Institute
Combination of Allosteric and Orthosteric EGFR Inhibitors for Treating Non-Small-Cell Lung Cancer.
ACS Med Chem Lett 15: 342-343 (2024)
Smith, Gambrell & Russell
Novel Tetrahydropyrido[3,4-
ACS Med Chem Lett 15: 318-319 (2024)
Smith, Gambrell & Russell
Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain.
ACS Med Chem Lett 15: 355-361 (2024)
University of Zurich
Synthesis and Biophysical Characterization of Fingolimod Derivatives as Cardiac Troponin Antagonists.
ACS Med Chem Lett 15: 413-417 (2024)
King'S College London
Novel AT2R Antagonists for Treating Chronic Pain.
ACS Med Chem Lett 15: 326-327 (2024)
Smith, Gambrell & Russell
Discovery of novel itaconimide-based derivatives as potent HDAC inhibitors for the efficient treatment of prostate cancer.
Eur J Med Chem 269:
China Pharmaceutical University
Insights from structure-activity relationships and the binding mode of peptidic α-ketoamide inhibitors of the malaria drug target subtilisin-like SUB1.
Eur J Med Chem 269:
University of Paris
Identification of Novel Series of Potent and Selective Relaxin Family Peptide Receptor 1 (RXFP1) Agonists.
J Med Chem 67: 4442-4462
AstraZeneca
Structure-Guided Discovery of Potent and Selective CLK2 Inhibitors for the Treatment of Knee Osteoarthritis.
J Med Chem 67: 4603-4623
China Pharmaceutical University
Discovery of Conformationally Constrained ALK2 Inhibitors.
J Med Chem 67: 4707-4725
Ontario Institute for Cancer Research
Design and Synthesis of 3-(2H-Chromen-3-yl)-5-aryl-1,2,4-oxadiazole Derivatives as Novel Toll-like Receptor 2/1 Agonists That Inhibit Lung Cancer In Vitro and In Vivo.
J Med Chem 67: 4583-4602
Beijing Institute of Radiation Medicine
RNA-Small-Molecule Interaction: Challenging the "Undruggable" Tag.
J Med Chem 67: 4259-4297
Panjab University
Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors.
Bioorg Med Chem 103:
Insilico Medicine Shanghai Ltd
Novel pyrrole based CB2 agonists: New insights on CB2 receptor role in regulating neurotransmitters' tone.
Eur J Med Chem 269:
University of Salerno
Inhibition of cancer cells by Quinoline-Based compounds: A review with mechanistic insights.
Bioorg Med Chem 103:
Amity University
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity.
Eur J Med Chem 269:
German University in Cairo
Targeting kelch-like (KLHL) proteins: achievements, challenges and perspectives.
Eur J Med Chem 269:
China Pharmaceutical University
Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model.
J Med Chem 67: 4855-4869
Shanghai University of Traditional Chinese Medicine
Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation.
J Med Chem 67: 4739-4756
Shenyang Pharmaceutical University
Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury.
J Med Chem 67: 4889-4903
Fujian University of Traditional Chinese Medicine
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy.
Eur J Med Chem 269:
South Valley University
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.
Eur J Med Chem 269:
Ningxia Medical University
Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations.
J Med Chem 67: 4346-4375
Nanjing University of Chinese Medicine
Terpenes and Terpenoids Conjugated with BODIPYs: An Overview of Biological and Chemical Properties.
J Nat Prod 87: 1306-1319 (2024)
Palacky University
Discovery and Characterization of a New Class of C5aR1 Antagonists Showing In Vivo Activity.
J Med Chem 67: 4100-4119
Idorsia Pharmaceuticals
Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability.
J Med Chem 67: 5032-5052
Shandong University
Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases.
Eur J Med Chem 269:
University of Sussex
Discovery of 5-aminopyrido[2,3-d]pyrimidin-7(8H)-one derivatives as new hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Eur J Med Chem 269:
Shanghai Institute of Organic Chemistry
Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs.
J Med Chem 67: 4641-4654
Imperial College London
Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression.
J Med Chem 67: 5275-5304
University of Michigan
Mechanism-Based Macrocyclic Inhibitors of Serine Proteases.
J Med Chem 67: 4833-4854
Washington University School of Medicine
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
J Med Chem 67: 4936-4949 (2024)
Mirati Therapeutics
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
J Med Chem 67: 4916-4935
China Pharmaceutical University
Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor.
J Med Chem 67: 5093-5108
Novartis Pharma
Sulfone-based human liver pyruvate kinase inhibitors - Design, synthesis and in vitro bioactivity.
Eur J Med Chem 269:
University of Gothenburg
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
J Med Chem 67: 4691-4706 (2024)
Max Planck Institute of Molecular Physiology
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation.
J Med Chem 67: 4819-4832
Genentech
The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
J Med Chem 67: 4676-4690
Biogen
Development of a Series of Pyrrolopyridone MAT2A Inhibitors.
J Med Chem 67: 4541-4559
AstraZeneca
Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus.
J Med Chem 67: 4757-4781
Sichuan University
Discovery of Novel PD-L1 Small-Molecular Inhibitors with Potent In Vivo Anti-tumor Immune Activity.
J Med Chem 67: 4977-4997
China Pharmaceutical University
Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2).
J Med Chem 67: 4655-4675
Astex Pharmaceuticals
Discovery of N-benzylbenzamide-based allosteric inhibitors of Aurora kinase A.
Bioorg Med Chem 102:
Korea Institute of Science and Technology (KIST)
Novel thiazolidin-4-one benzenesulfonamide hybrids as PPARγ agonists: Design, synthesis and in vivo anti-diabetic evaluation.
Eur J Med Chem 269:
National Research Centre
Structure-based discovery of potent CARM1 inhibitors for colorectal cancer therapy.
Eur J Med Chem 269:
East China Normal University
Biochemical and structural characterization of chlorhexidine as an ATP-assisted inhibitor against type 1 methionyl-tRNA synthetase from Gram-positive bacteria.
Eur J Med Chem 268:
Sun Yat-sen University
Drug-drug conjugates of MEK and Akt inhibitors for RAS-mutant cancers.
Bioorg Med Chem 102:
Kanazawa University
Casitas b cell lymphoma‑B (Cbl-b): A new therapeutic avenue for small-molecule immunotherapy.
Bioorg Med Chem 102:
China Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationship of Novel Pyridazinone-Based PARP7/HDACs Dual Inhibitors for Elucidating the Relationship between Antitumor Immunity and HDACs Inhibition.
J Med Chem 67: 4950-4976
Hangzhou Normal University
Optimizing drug-like properties of selective butyrylcholinesterase inhibitors for cognitive improvement: Enhancing aqueous solubility by disrupting molecular plane.
Eur J Med Chem 268:
China Pharmaceutical University
Research progress of DDR1 inhibitors in the treatment of multiple human diseases.
Eur J Med Chem 268:
Sichuan University
Design and biological evaluation of dual tubulin/HDAC inhibitors based on millepachine for treatment of prostate cancer.
Eur J Med Chem 268:
China Pharmaceutical University
The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364.
Eur J Med Chem 268:
China Pharmaceutical University
Cardiac Troponin Activator CK-963 Increases Cardiac Contractility in Rats.
J Med Chem 67: 7859-7869
Cytokinetics, Inc.
Identification of two novel chemical classes of Autotaxin (ATX) inhibitors using Enalos Asclepios KNIME nodes.
Bioorg Med Chem Lett 103: (2024)
Bsrc Alexander Fleming
Design, synthesis and anti-necroptosis activity of fused heterocyclic MLKL inhibitors.
Bioorg Med Chem 102:
Ningxia Medical University
Discovery of RORγ Allosteric Fluorescent Probes and Their Application: Fluorescence Polarization, Screening, and Bioimaging.
J Med Chem 67: 4194-4224
Nanjing University of Chinese Medicine
Dual Inhibitors of Brain Carbonic Anhydrases and Monoamine Oxidase-B Efficiently Protect against Amyloid-β-Induced Neuronal Toxicity, Oxidative Stress, and Mitochondrial Dysfunction.
J Med Chem 67: 4170-4193
University of Florence
Amide Alkaloids as Privileged Sources of Senomodulators for Therapeutic Purposes in Age-Related Diseases.
J Nat Prod 87: 617-628 (2024)
Sorbonne University
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment.
Eur J Med Chem 268:
Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of selective covalent inhibitors of FGFR4.
Eur J Med Chem 268:
Central South University
Insight into small-molecule inhibitors targeting extracellular nucleotide pyrophosphatase/phosphodiesterase1 for potential multiple human diseases.
Eur J Med Chem 268:
Sichuan University
Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease.
Eur J Med Chem 268:
Emory University
Current advances and development strategies of targeting son of sevenless 1 (SOS1) in drug discovery.
Eur J Med Chem 268:
Sichuan University
Structural Basis for Molecular Recognition of Cannabinoids by Inhibitory Cys-Loop Channels.
J Med Chem 67: 3274-3286
Universidad de Buenos Aires
Discovery of a novel class of reversible monoacylglycerol lipase inhibitors for potential treatment of depression.
Eur J Med Chem 268:
China Pharmaceutical University
Structure-Based Discovery of High-Affinity Small Molecule Ligands and Development of Tool Probes to Study the Role of Chitinase-3-Like Protein 1.
J Med Chem 67: 3959-3985
Molecure
Microascones, Decahydrofluorene-Class Alkaloids from the Marine-Derived Fungus
J Nat Prod 87: 810-819 (2024)
Chinese Academy of Sciences
Synthesis, SARS-CoV-2 main protease inhibition, molecular docking and in silico ADME studies of furanochromene-quinoline hydrazone derivatives.
Bioorg Med Chem Lett 102:
Susquehanna University
Small-molecule agents for treating skin diseases.
Eur J Med Chem 268:
Hangzhou Normal University
Fragment growth-based discovery of novel TNIK inhibitors for the treatment of colorectal cancer.
Eur J Med Chem 268:
Sichuan University
Synthesis and biological evaluation of triazolones/oxadiazolones as novel urease inhibitors.
Bioorg Med Chem 102:
Jishou University
Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors.
J Med Chem 67: 3813-3842
Goethe University Frankfurt
Unleashing the Potential of Camptothecin: Exploring Innovative Strategies for Structural Modification and Therapeutic Advancements.
J Med Chem 67: 3244-3273
Southwest Jiaotong University
The discovery of novel and potent indazole NLRP3 inhibitors enabled by DNA-encoded library screening.
Bioorg Med Chem Lett 102:
BioAge Labs
Sokotrasterol Sulfate Suppresses IFN-γ-Induced PD-L1 Expression by Inhibiting JAK Activity.
J Nat Prod 87: 713-721 (2024)
Fudan University
Discovery and Structure-Activity Relationships of Novel ssDAF-12 Receptor Modulators.
J Med Chem 67: 4150-4169
University of Perugia
Design, Synthesis, and Biological Evaluation of Pierardine Derivatives as Novel Brain-Penetrant and In Vivo Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
J Med Chem 67: 3358-3384
Anhui University of Chinese Medicine
Discovery of potent small molecule inhibitors of histone lysine methyltransferase NSDs.
Eur J Med Chem 268:
Jiangsu University of Technology
Design, Synthesis, and Antitumor Activity Evaluation of Novel VISTA Small Molecule Inhibitors.
J Med Chem 67: 3590-3605
China Pharmaceutical University
Fyn, Blk, and Lyn kinase inhibitors: A mini-review on medicinal attributes, research progress, and future insights.
Bioorg Med Chem Lett 102:
ISF College of Pharmacy
Development of 1,5-diarylpyrazoles as EGFR/JNK-2 dual inhibitors: design, synthesis, moleecular docking, and bioactivity evaluation.
Bioorg Med Chem Lett 102:
Al-Azhar University
Optimization Efforts for Identification of Novel Highly Potent Keap1-Nrf2 Protein-Protein Interaction Inhibitors.
J Med Chem 67: 3741-3763
Japan Tobacco
Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich
J Nat Prod 87: 722-732 (2024)
University of Naples Federico Ii
Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer.
J Med Chem 67: 3339-3357
National Institute of Pharmaceutical Education and Research-Ahmedabad (NIPER-A)
Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study.
Bioorg Med Chem 101: (2024)
University of Belgrade-Institute of Chemistry
Research progress of LSD1-based dual-target agents for cancer therapy.
Bioorg Med Chem 101: (2024)
Xinxiang University
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
Bioorg Med Chem 101: (2024)
University of Sharjah
Novel sulfonamide-indolinone hybrids targeting mitochondrial respiration of breast cancer cells.
Eur J Med Chem 268:
Ain Shams University
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability.
Eur J Med Chem 268:
Hanyang University
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design.
Bioorg Med Chem 101: (2024)
Bristol Myers Squibb
Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity.
Eur J Med Chem 268:
University of Perugia
Antiviral Protein-Protein Interaction Inhibitors.
J Med Chem 67: 3205-3231 (2024)
Wroclaw University
Allosteric Activation of α7 Nicotinic Acetylcholine Receptors by Novel 2-Arylamino-thiazole-5-carboxylic Acid Amide Derivatives for the Improvement of Cognitive Deficits in Mice.
J Med Chem 67: 6344-6364
Qingdao University Medical College
Discovery of Novel Steroid-Based Histamine H3 Receptor Antagonists/Inverse Agonists.
J Med Chem 67: 3643-3667
Gedeon Richter Plc.
Discovery of dual-action phenolic 4-arylidene-isoquinolinones with antioxidant and α-glucosidase inhibition activities.
RSC Med Chem 15: 519-538 (2024)
National Autonomous University of Mexico
Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.
RSC Med Chem 15: 539-552 (2024)
Zhejiang University
Small molecule WDR5 inhibitors down-regulate lncRNA expression.
RSC Med Chem 15: 636-640 (2024)
Max Planck Institute of Molecular Physiology
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators.
RSC Med Chem 15: 607-611 (2024)
Dana-Farber Cancer Institute
Highly potent and selective phosphatidylinositol 4-kinase IIIβ inhibitors as broad-spectrum anti-rhinoviral agents.
RSC Med Chem 15: 704-719 (2024)
Korea Research Institute of Chemical Technology
Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.
RSC Med Chem 15: 399-415 (2024)
University of Arkansas
Role of heterocycles in inhibition of VEGFR-2 - a recent update (2019-2022).
RSC Med Chem 15: 416-432 (2024)
Srmpp
Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors.
RSC Med Chem 15: 733-752 (2024)
Health Affairs Directorate - Giza
Consensus screening for a challenging target: the quest for P-glycoprotein inhibitors.
RSC Med Chem 15: 720-732 (2024)
The Scripps Research Institute
Re-exploration of tetrahydro-β-carboline scaffold: Discovery of selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting and neuroprotective activities.
Bioorg Med Chem Lett 102:
Yangling Vocational & Technical College
Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-2.
Bioorg Med Chem Lett 101: (2024)
Southern Medical University
Identification of 3-aryl-5-methyl-isoxazole-4-carboxamide derivatives and analogs as novel HIF-2α agonists through docking-based virtual screening and structural modification.
Eur J Med Chem 268:
Zhejiang University
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
J Med Chem 67: 3986-4006
Shanghai Institute of Materia Medica
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
J Med Chem 67: 3400-3418
Merck & Co.
Design and Synthesis of Dual-Target Inhibitors Targeting Androgen Receptors and Glucocorticoid Receptors to Overcome Antiandrogen Resistance in Castration-Resistant Prostate Cancer.
J Med Chem 67: 3419-3436
Zhejiang Normal University
Hit-to-Lead Identification and Validation of a Triaromatic Pleuromutilin Antibiotic Candidate.
J Med Chem 67: 3692-3710
University of Southern Denmark
Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis.
J Med Chem 67: 3571-3589
Bristol Myers Squibb
Synthesis and kinetic evaluation of phosphomimetic inhibitors targeting type B ribose-5-phosphate isomerase from Mycobacterium tuberculosis.
Bioorg Med Chem Lett 102:
Universita Paris-Saclay
Targeting insulin-like growth factor 2 mRNA-binding proteins (IGF2BPs) for the treatment of cancer.
Eur J Med Chem 268:
China Pharmaceutical University
Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition.
Eur J Med Chem 268:
Zhejiang University
Discovery of 5-Hydroxy-1,4-naphthoquinone (Juglone) Derivatives as Dual Effective Agents Targeting Platelet-Cancer Interplay through Protein Disulfide Isomerase Inhibition.
J Med Chem 67: 3626-3642 (2024)
National Taiwan University
Design, synthesis, biological evaluation and in silico studies of novel quinoline derivatives as potential radioprotective molecules targeting the TLR2 and p53 pathways.
Eur J Med Chem 268:
Guangdong Pharmaceutical University
Design, synthesis and biological evaluation of novel 1,2,4a,5-tetrahydro-4H-benzo[b][1,4]oxazino[4,3-d][1,4]oxazine-based AAK1 inhibitors with anti-viral property against SARS-CoV-2.
Eur J Med Chem 268:
Hangzhou Normal University
Discovery of Novel N-(Anthracen-9-ylmethyl) Benzamide Derivatives as ZNF207 Inhibitors Promising in Treating Glioma.
J Med Chem 67: 3909-3934
China Pharmaceutical University
Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment.
J Med Chem 67: 3504-3519
Chinese Academy of Medical Sciences and Peking Union Medical College
A Survey of Recently Discovered Naturally Occurring Organohalogen Compounds.
J Nat Prod 87: 1285-1305 (2024)
Dartmouth College
Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors.
J Med Chem 67: 3606-3625
China Pharmaceutical University
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor.
Bioorg Med Chem Lett 101: (2024)
Tianjin University
α-Amino bisphosphonate triazoles serve as GGDPS inhibitors.
Bioorg Med Chem Lett 102:
University of Iowa
Rational Design of Benzobisheterocycle Metallo-β-Lactamase Inhibitors: A Tricyclic Scaffold Enhances Potency against Target Enzymes.
J Med Chem 67: 3795-3812
University of the Republic (UdelaR)
Pyrazolamide derivatives inhibit α-Synuclein aggregation, disaggregate preformed fibers, and reduce inclusion formation in neuron cells.
Eur J Med Chem 268:
Zhengzhou University
Does size matter? - Comparing pyranoses with septanoses as ligands of the bacterial lectin FimH.
Eur J Med Chem 268:
University of Basel
Novel estrogen receptor β/histone deacetylase dual-targeted near-infrared fluorescent probes as theranostic agents for imaging and treatment of prostate cancer.
Eur J Med Chem 268:
Zhongnan Hospital of Wuhan University
Discovery of novel pyrrolo[2,3-d]pyrimidines as potent menin-mixed lineage leukemia interaction inhibitors.
Eur J Med Chem 268:
Xi'an Jiaotong University
Identification of the exosomal PD-L1 inhibitor to promote the PD-1 targeting therapy of gastric cancer.
Eur J Med Chem 268:
The First Affiliated Hospital of Zhengzhou University
Discovery of a Potent Nicotinamide Phosphoribosyltransferase Activator for Improving Aging-associated Dysfunctions.
J Med Chem 67: 4120-4130
Second Military Medical University (Naval Medical University)
Design, synthesis and biological evaluation of CDC20 inhibitors for treatment of triple-negative breast cancer.
Eur J Med Chem 268:
China Pharmaceutical University
Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer.
Eur J Med Chem 268:
University of Turin
Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Bioorg Med Chem 101: (2024)
Shenyang Pharmaceutical University
Glycan-Modified Peptides for Dual Inhibition of Human Immunodeficiency Virus Entry into Dendritic Cells and T Cells.
J Med Chem 67: 4225-4233
Chinese Academy of Sciences
Heterocyclic-Modified Imidazoquinoline Derivatives: Selective TLR7 Agonist Regulates Tumor Microenvironment against Melanoma.
J Med Chem 67: 3321-3338
Southern Medical University
PSMA-targeted SMART molecules outfitted with SN38.
Bioorg Med Chem Lett 101: (2024)
Washington State University
2-Phenylcyclopropylmethylamine (PCPMA) as a privileged scaffold for central nervous system drug design.
Bioorg Med Chem Lett 101: (2024)
Shanghaitech University
Ecto-nucleotide pyrophosphatase/phosphodiesterase 1 inhibitors: Research progress and prospects.
Eur J Med Chem 267:
China Pharmaceutical University
Overview of the development of protein arginine methyltransferase modulators: Achievements and future directions.
Eur J Med Chem 267:
China Pharmaceutical University
Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity.
Eur J Med Chem 267:
University of South China
Discovery of Effective Dual PROTAC Degraders for Neurodegenerative Disease-Associated Aggregates.
J Med Chem 67: 3448-3466
Sun Yat-sen University
Synthesis and Evaluation of Natural and Unnatural Tetrahydrocannabiorcol for Its Potential Use in Neuropathologies.
J Nat Prod 87: 167-175 (2024)
Csir-Indian Institute of Integrative Medicine
Discovery of N-(1-(2-hydroxyethyl)quinolin-2-one)-N'-(1-phenyl-1H-pyrazol-5-yl)methyl) urea as Mode-Selective TRPV1 antagonist.
Bioorg Med Chem Lett 101: (2024)
Seoul National University
Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in vivo.
Eur J Med Chem 267:
Sichuan University
Design, Synthesis, and Activity Evaluation of Fluorine-Containing Scopolamine Analogues as Potential Antidepressants.
J Med Chem 67: 5391-5420
Henan Normal University
Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.
ACS Med Chem Lett 15: 302-309 (2024)
Vanderbilt University
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.
ACS Med Chem Lett 15: 189-196 (2024)
Bristol Myers Squibb
Novel Fused Triazole Compounds as RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases.
ACS Med Chem Lett 15: 177-178 (2024)
Smith, Gambrell & Russell
3-Alkynyl Carboxamides as AEP Modulators for Treating Alzheimer's Disease.
ACS Med Chem Lett 15: 159-160 (2024)
Smith, Gambrell & Russell
Synthesis and Structural Optimization of ATG4B Inhibitors for the Attenuation of Autophagy in Glioblastoma.
ACS Med Chem Lett 15: 258-264 (2024)
Northwestern University
Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP).
ACS Med Chem Lett 15: 270-279 (2024)
Nanjing University of Chinese Medicine
Innovative Therapeutic Strategies in TYK2-Targeted Treatments: From Cancer to Autoimmune Disorders.
ACS Med Chem Lett 15: 174-176 (2024)
Usona Institute
Novel PARP1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 15: 161-162 (2024)
Smith, Gambrell & Russell
Nicotinamide Phosphoribosyltransferase Positive Allosteric Modulators Attenuate Neuronal Oxidative Stress.
ACS Med Chem Lett 15: 205-214 (2024)
University of Illinois At Chicago
Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2.
ACS Med Chem Lett 15: 250-257 (2024)
University of Florence
Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.
ACS Med Chem Lett 15: 181-188 (2024)
Bristol-Myers Squibb Research & Development
The Bis(1,2,3,4-tetrahydroisoquinoline) Alkaloids Cepharanthine and Berbamine Are Ligands of SK Channels.
ACS Med Chem Lett 15: 215-220 (2024)
University of Liege
Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis.
ACS Med Chem Lett 15: 163-164 (2024)
Smith, Gambrell & Russell
Discovery of a novel series of pyridone amides as Na
Bioorg Med Chem Lett 101: (2024)
Sichuan University
Discovery of novel, potent, selective and orally bioavailable HPK1 inhibitor for enhancing the efficacy of anti-PD-L1 antibody.
Eur J Med Chem 267:
Hangzhou Medical College
Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma.
J Med Chem 67: 2884-2906
Shanghai Institute of Materia Medica
Discovery of the Novel, Orally Active, and Selective LPA1 Receptor Antagonist ACT-1016-0707 as a Preclinical Candidate for the Treatment of Fibrotic Diseases.
J Med Chem 67: 2397-2424
Idorsia Pharmaceuticals, Ltd
Discovery of Highly Potent Small-Molecule PD-1/PD-L1 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
J Med Chem 67: 4083-4099
China Pharmaceutical University
Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J Med Chem 67: 2667-2689
Jinan University
BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor.
J Med Chem 67: 2907-2940
Bayer AG
Design, synthesis of new 3H-imidazo[4,5-b]pyridine derivatives and evaluation of their inhibitory properties as mixed lineage kinase 3 inhibitors.
Bioorg Med Chem Lett 101: (2024)
Chungnam National University
Rational design, synthesis and biological evaluation of novel HIV-1 protease inhibitors containing 2-phenylacetamide derivatives as P2 ligands with potent activity against DRV-Resistant HIV-1 variants.
Bioorg Med Chem Lett 101: (2024)
Xuzhou Medical University
Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells.
Bioorg Med Chem 100:
Kyoto Prefectural University of Medicine
Anticancer mechanism of coumarin-based derivatives.
Eur J Med Chem 267:
Tribhuvan University
MYC the oncogene from hell: Novel opportunities for cancer therapy.
Eur J Med Chem 267:
Biomedical Research Foundation of the Academy of Athens
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors.
Eur J Med Chem 267:
Purdue University
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
J Med Chem 67: 2369-2378 (2024)
Calibr At Scripps Research Institute
Discovery of Anti-Hypercholesterolemia Agents Targeting LXRα from Marine Microorganism-Derived Natural Products.
J Nat Prod 87: 322-331 (2024)
Guangxi University of Chinese Medicine
Design, synthesis and biological evaluation of 2-phenylaminopyrimidine derivatives as EGFR inhibitors.
Bioorg Med Chem Lett 101: (2024)
Jiangnan University
Tackling Influenza A virus by M2 ion channel blockers: Latest progress and limitations.
Eur J Med Chem 267:
National Institute of Pharmaceutical Education and Research-Hyderabad
Colony Stimulating Factor-1 Receptor: An emerging target for neuroinflammation PET imaging and AD therapy.
Bioorg Med Chem 100:
Graphic Era Hill University
Discovery of small molecule benzothiazole and indole derivatives tackling tau 2N4R and α-synuclein fibrils.
Bioorg Med Chem 100:
Purdue University
Discovery and Characterization of Selective, First-in-Class Inhibitors of Citron Kinase.
J Med Chem 67: 2631-2666
Lerner Research Institute
Discovery of a Novel Series of Homo sapiens Caseinolytic Protease P Agonists for Colorectal Adenocarcinoma Treatment via ATF3-Dependent Integrated Stress Response.
J Med Chem 67: 2812-2836
Sichuan University
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.
J Med Chem 67: 3112-3126
Incyte
Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment.
Eur J Med Chem 267:
China Pharmaceutical University
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management.
Eur J Med Chem 267:
Henan University
Design, Synthesis, and Biological Evaluation of Dual Inhibitors of EGFRL858R/T790M/ACK1 to Overcome Osimertinib Resistance in Nonsmall Cell Lung Cancers.
J Med Chem 67: 2777-2801
Sichuan University
Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases.
J Med Chem 67: 2438-2465
The People's Hospital of Guangxi Zhuang Autonomous Region & Guangxi Academy of Medical Sciences
Identification of novel benzothiazole derivatives as inhibitors of NEDDylation pathway to inhibit the progression of gastric cancer.
Bioorg Med Chem Lett 100:
Zhengzhou University
Norterpene Cyclic Peroxides from the Marine Sponge
J Nat Prod 87: 358-364 (2024)
Korea Institute of Ocean Science and Technology
Synthesis and biological evaluation of 1H-pyrrolo[3,2-g]isoquinolines.
Bioorg Med Chem 100:
Universite Clermont Auvergne
A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRASG12C Inhibitor.
J Med Chem 67: 2487-2511
Ocean University of China
Identification of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffolds as potent Lck inhibitors as anti-cancer agents.
Bioorg Med Chem Lett 102:
Korea Institute of Science and Technology
Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma.
J Med Chem 67: 2466-2486
Fudan University
Discovery of D25, a Potent and Selective MNK Inhibitor for Sepsis-Associated Acute Spleen Injury.
J Med Chem 67: 3167-3189
Shandong First Medical University
Exploring 2-methyl-substituted vitamin K3 derivatives with potent inhibitory activity against the 3CL protease of SARS-CoV-2.
Bioorg Med Chem Lett 100:
Shibaura Institute of Technology
Research progress on small molecule inhibitors targeting KRAS G12C with acrylamide structure and the strategies for solving KRAS inhibitor resistance.
Bioorg Med Chem 100:
Jiangxi Science & Technology Normal University
pH regulators and their inhibitors in tumor microenvironment.
Eur J Med Chem 267:
University of South China
Design, synthesis, and biological characterization of proteolysis targeting chimera (PROTACs) for the ataxia telangiectasia and RAD3-related (ATR) kinase.
Eur J Med Chem 267:
Martin-Luther-University of Halle-Wittenberg
Identification of (4-chlorophenyl)(5-hydroxynaphtho[1,2-b]furan-3-yl)methanone as novel COX-2 inhibitor with analgesic profile.
Bioorg Med Chem Lett 100:
Sichuan University
Discovery of a novel series of selective macrocyclic PKCTheta inhibitors.
Bioorg Med Chem Lett 100:
Galderma SA
Exploring the Function of (+)-Naltrexone Precursors: Their Activity as TLR4 Antagonists and Potential in Treating Morphine Addiction.
J Med Chem 67: 3127-3143
Chinese Academy of Sciences
Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.
J Med Chem 67: 3039-3065
Symeres
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
J Med Chem 67: 3090-3111
AstraZeneca
Structure-based discovery of a new series of nucleoside-derived ring-opening PRMT5 inhibitors.
Eur J Med Chem 267:
University of Chinese Academy of Sciences
Identifying Marine-Derived Tanzawaic Acid Derivatives as Novel Inhibitors against Osteoclastogenesis and Osteoporosis via Downregulation of NF-κB and NFATc1 Activation.
J Med Chem 67: 2602-2618
Chinese Academy of Sciences
Synthetic Approaches to Novel Human Carbonic Anhydrase Isoform Inhibitors Based on Pyrrol-2-one Moiety.
J Med Chem 67: 3018-3038 (2024)
Romanian Academy
Discovery of 2,3-Diaminoindole Derivatives as a Novel Class of NOD Antagonists.
J Med Chem 67: 3004-3017
University of Naples "Federico II"
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
J Med Chem 67: 2321-2336 (2024)
Nurix Therapeutics
ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases.
J Med Chem 67: 2837-2848
Stanford University
Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500).
J Med Chem 67: 2349-2368
Repare Therapeutics, Inc.
Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.
J Med Chem 67: 2712-2731
University of Illinois at Chicago
Targeting autophagy drug discovery: Targets, indications and development trends.
Eur J Med Chem 267:
China Jiliang University
Synthesis and biological evaluation of selective Pepstatin based trifluoromethylated inhibitors of Cathepsin D.
Eur J Med Chem 267:
CY Cergy Paris Universite
Design, Synthesis, and Biological Evaluation for First GPX4 and CDK Dual Inhibitors.
J Med Chem 67: 2758-2776
China Pharmaceutical University
Discovery of thiophen-2-ylmethylene bis-dimedone derivatives as novel WRN inhibitors for treating cancers with microsatellite instability.
Bioorg Med Chem 100:
Korea University
Identification of Piperazinyl-Difluoro-indene Derivatives Containing Pyridyl Groups as Potent FGFR Inhibitors against FGFR Mutant Tumor: Design, Synthesis, and Biological Evaluation.
J Med Chem 67: 2941-2962
Peking Union Medical College and Chinese Academy of Medical Sciences
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate.
J Med Chem 67: 4525-4540 (2024)
University of Oxford
Neopetrotaurines A-C, Isoquinoline Alkaloids with an Unprecedented Taurine Bridge from the Sponge
J Nat Prod 87: 332-339 (2024)
National Cancer Institute
PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
J Med Chem 67: 2619-2630 (2024)
Unidad Bics
Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research.
J Med Chem 67: 1701-1733
Bristol-Myers Squibb
Discovery of new piperaquine hybrid analogs linked by triazolopyrimidine and pyrazolopyrimidine scaffolds with antiplasmodial and transmission blocking activities.
Eur J Med Chem 267:
Fundacao Oswaldo Cruz
Fragment-to-Lead Medicinal Chemistry Publications in 2022.
J Med Chem 67: 2287-2304
Astex Pharmaceuticals
Discovery of Artemisinins as Microsomal Prostaglandins Synthase-2 Inhibitors for the Treatment of Colorectal Cancer via Chemoproteomics.
J Med Chem 67: 2083-2094
Changshu Institute of Technology
First-in-Class Dual EZH2-HSP90 Inhibitor Eliciting Striking Antiglioblastoma Activity
J Med Chem 67: 2963-2985 (2024)
Taipei Medical University
Discovery and Characterization of a Bicyclic Peptide (Bicycle) Binder to Thymic Stromal Lymphopoietin.
J Med Chem 67: 2220-2235
BicycleTx Limited
Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats.
RSC Med Chem 15: 344-354 (2024)
Idorsia Pharmaceuticals
A survey of stapling methods to increase affinity, activity, and stability of ghrelin analogues.
RSC Med Chem 15: 254-266 (2024)
University of Western Ontario
The development of thymol-isatin hybrids as broad-spectrum antibacterial agents with potent anti-MRSA activity.
RSC Med Chem 15: 234-253 (2024)
Guru Nanak Dev University
Discovery of a dual-acting inhibitor of interleukin-1β and STATs for the treatment of inflammatory bowel disease.
RSC Med Chem 15: 193-206 (2024)
Guangzhou Medical University
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery.
RSC Med Chem 15: 70-80 (2024)
Shandong University
Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents:
RSC Med Chem 15: 293-308 (2024)
Misr International University
Physicochemical characterization of
RSC Med Chem 15: 119-126 (2024)
Tokyo Medical and Dental University
Highly efficient, catalyst-free, one-pot sequential four-component synthesis of novel spiroindolinone-pyrazole scaffolds as anti-Alzheimer agents:
RSC Med Chem 15: 207-222 (2024)
Persian Gulf University
Scaffold hopping based designing of selective ALDH1A1 inhibitors to overcome cyclophosphamide resistance: synthesis and biological evaluation.
RSC Med Chem 15: 309-321 (2024)
Punjabi University
Latest developments in coumarin-based anticancer agents: mechanism of action and structure-activity relationship studies.
RSC Med Chem 15: 10-54 (2024)
Csir-Central Glass & Ceramic Research Institute
Annual review of PROTAC degraders as anticancer agents in 2022.
Eur J Med Chem 267:
Zhengzhou University
Novel xanthone derivatives as potent sirtuin 2 inhibitors.
Bioorg Med Chem Lett 100:
Jagiellonian University Medical College
Novel small molecule inhibitors targeting renal cell carcinoma: Status, challenges, future directions.
Eur J Med Chem 267:
Sichuan University
Discovery of matrix metalloproteinase inhibitors as anti-skin photoaging agents.
Eur J Med Chem 267:
Hangzhou Normal University
Discovery of tricyclic PARP7 inhibitors with high potency, selectivity, and oral bioavailability.
Eur J Med Chem 266:
Hubei Polytechnic University
Peptide-Drug Conjugates: An Emerging Direction for the Next Generation of Peptide Therapeutics.
J Med Chem 67: 1641-1661
University of Illinois Chicago
Design, synthesis and evaluate of indazolylaminoquinazoline derivatives as potent Tropomyosin receptor kinase (TRK) inhibitors.
Bioorg Med Chem 99:
Shanghai Institute of Pharmaceutical Industry Co., Ltd
Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
J Med Chem 67: 1734-1746
Kinnate Biopharma
Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitors.
Bioorg Med Chem Lett 100:
IRBM S.p.A.
Hybrids of selective COX-2 inhibitors and active derivatives of edaravone as COX-2 selective NSAIDs with free radical scavenging activity: Design, synthesis and biological activities.
Eur J Med Chem 266:
China Pharmaceutical University
Novel Carbonic Anhydrase Inhibitors with Dual-Tail Core Sulfonamide Show Potent and Lasting Effects for Glaucoma Therapy.
J Med Chem 67: 3066-3089
University of Florence
Tight-Binding Small-Molecule Carboxylesterase 2 Inhibitors Reduce Intracellular Irinotecan Activation.
J Med Chem 67: 2019-2030
University of Toronto Mississauga
Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling.
Bioorg Med Chem 99:
University of Oxford
Recent advances in the development of deubiquitinases inhibitors as antitumor agents.
Eur J Med Chem 266:
China Pharmaceutical University
Design and synthesis of 4-amino-2',4'-dihydroxyindanone derivatives as potent inhibitors of tyrosinase and melanin biosynthesis in human melanoma cells.
Eur J Med Chem 266:
University of Grenoble Alpes
SIRT3 Activation a Promise in Drug Development? New Insights into SIRT3 Biology and Its Implications on the Drug Discovery Process.
J Med Chem 67: 1662-1689
Sapienza University of Rome
Multitargeting HDAC Inhibitors Containing a RAS/RAF Protein Interfering Unit.
J Med Chem 67: 2066-2082
Southeast University
Synthesis and biological evaluation of novel 18F-labeled 2,4-diaminopyrimidine derivatives for detection of ghrelin receptor in the brain.
Bioorg Med Chem Lett 99:
Kyoto University
Specific Inhibitors of Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity.
J Med Chem 67: 1843-1860
University of Bayreuth
3,5-Disubstituted-thiazolidine-2,4-dione hybrids as antidiabetic agents: Design, synthesis, in-vitro and In vivo evaluation.
Eur J Med Chem 266:
IK Gujral Punjab Technical University
Rebamipide and Derivatives are Potent, Selective Inhibitors of Histidine Phosphatase Activity of the Suppressor of T Cell Receptor Signaling Proteins.
J Med Chem 67: 1949-1960
University of Minnesota
Development of UTX-143, a selective sodium-hydrogen exchange subtype 5 inhibitor, using amiloride as a lead compound.
Bioorg Med Chem 99:
Tokushima University
Structure-based design and synthesis of sulfonylureas as novel NLRP3 inhibitors for Alzheimer's disease.
Bioorg Med Chem Lett 99:
Chonnam National University
In vitro and in vivo anti-pigmentation effects of 2-mercaptobenzimidazoles as nanomolar tyrosinase inhibitors on mammalian cells and zebrafish embryos: Preparation of pigment-free zebrafish embryos.
Eur J Med Chem 266:
Pusan National University
Drug discovery targeting nicotinamide phosphoribosyltransferase (NAMPT): Updated progress and perspectives.
Bioorg Med Chem 99:
China Pharmaceutical University
Inhibition of dengue viruses by N-methylcytisine thio derivatives through targeting viral envelope protein and NS2B-NS3 protease.
Bioorg Med Chem Lett 99:
Kuang Tien General Hospital
Fluorinated captopril analogues inhibit metallo-β-lactamases and facilitate structure determination of NDM-1 binding pose.
Eur J Med Chem 266:
UiT The Arctic University of Norway
Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization.
J Med Chem 67: 1758-1782
University of Siena
Development of a tetrahydroindazolone-based HDAC6 inhibitor with in-vivo anti-arthritic activity.
Bioorg Med Chem 99:
Sungkyunkwan University
Structure-Guided Design of a Highly Potent Partial RXR Agonist with Superior Physicochemical Properties.
J Med Chem 67: 2152-2164
Ludwig-Maximilians-Universitat (LMU) Munchen
Design and Synthesis of Dual-Targeting Inhibitors of sEH and HDAC6 for the Treatment of Neuropathic Pain and Lipopolysaccharide-Induced Mortality.
J Med Chem 67: 2095-2117
Shenyang Pharmaceutical University
Development of potent and selective ULK1/2 inhibitors based on 7-azaindole scaffold with favorable in vivo properties.
Eur J Med Chem 266:
H. Lee Moffitt Cancer Center and Research Institute
Drug discovery and optimization based on the co-crystal structure of natural product with target.
Eur J Med Chem 266:
Anhui Medical University
Peptidomimetics as potent dual SARS-CoV-2 cathepsin-L and main protease inhibitors: In silico design, synthesis and pharmacological characterization.
Eur J Med Chem 266:
University of Salerno
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis.
J Med Chem 67: 1914-1931
Zhejiang University
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
J Med Chem 67: 1747-1757
Kinnate Biopharma
Solubilizer Tag Effect on PD-L1/Inhibitor Binding Properties for
ACS Med Chem Lett 15: 36-44 (2024)
Jagiellonian University
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
ACS Med Chem Lett 15: 123-131 (2024)
Merck
Discovery of Malarial Threonyl tRNA Synthetase Inhibitors by Screening of a Focused Fragment Library.
ACS Med Chem Lett 15: 76-80 (2024)
Latvian Institute of Organic Synthesis
Discovery of Novel PDEδ Autophagic Degraders: A Case Study of Autophagy-Tethering Compound (ATTEC).
ACS Med Chem Lett 15: 29-35 (2024)
East China University of Science and Technology
Synthesis, Antiacetylcholinesterase Activity, and Molecular Dynamics Simulation of Aporphine-benzylpyridinium Conjugates.
ACS Med Chem Lett 15: 132-142 (2024)
Chulabhorn Research Institute
Structure-Based Design and Evaluation of Reversible KRAS G13D Inhibitors.
ACS Med Chem Lett 15: 21-28 (2024)
Genentech
Chemical Catalysis Guides Structural Identification for the Major
ACS Med Chem Lett 15: 107-115 (2024)
Baylor College of Medicine
Positive Allosteric Modulators of alpha7 Nicotinic Acetylcholine Receptor for the Treatment of Several Central Nervous System Diseases.
ACS Med Chem Lett 15: 6-8 (2024)
Therachem Research Medilab
Novel Pyrazolopyridine Inhibitors of Monoacylglycerol Lipase for the Treatment of Neurodegenerative Diseases and Neuroinflammation.
ACS Med Chem Lett 15: 19-20 (2024)
Arrival Discovery
Design and synthesis of unique morphinan-type molecules: Their application to the search for the unexplored binding domain between opioid receptors and morphinan ligands.
Bioorg Med Chem Lett 99:
University of Tsukuba
Discovery of the First-in-Class RORγ Covalent Inhibitors for Treatment of Castration-Resistant Prostate Cancer.
J Med Chem 67: 1481-1499
Sun Yat-Sen University
Discovery, Optimization, and Evaluation of Novel Pyridin-2(1H)-one Analogues as Potent TRK Inhibitors for Cancer Treatment.
J Med Chem 67: 1168-1183
Shanghai Tech University
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
J Med Chem 67: 1500-1512
AstraZeneca
HDAC/NAMPT dual inhibitors overcome initial drug-resistance in p53-null leukemia cells.
Eur J Med Chem 266:
Ocean University of China
Therapeutic potential of Coumarin-polyphenolic acid hybrids in PD: Inhibition of α-Syn aggregation and disaggregation of preformed fibrils, leading to reduced neuronal inclusion formation.
Bioorg Med Chem Lett 99:
Zhengzhou University
A further pocket or conformational plasticity by mapping COX-1 catalytic site through modified-mofezolac structure-inhibitory activity relationships and their antiplatelet behavior.
Eur J Med Chem 266:
University of Bari "Aldo Moro"
Chromone-based small molecules for multistep shutdown of arachidonate pathway: Simultaneous inhibition of COX-2, 15-LOX and mPGES-1 enzymes.
Eur J Med Chem 266:
Alexandria University
Phenoxytacrine derivatives: Low-toxicity neuroprotectants exerting affinity to ifenprodil-binding site and cholinesterase inhibition.
Eur J Med Chem 266:
Charles University in Prague
Dual Antagonism of α9α10 nAChR and GABAB Receptor-Coupled CaV2.2 Channels by an Analgesic αO-Conotoxin Analogue.
J Med Chem 67: 971-987
Ocean University of China
Discovery of Novel Aminobutanoic Acid-Based ASCT2 Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.
J Med Chem 67: 988-1007
China Pharmaceutical University
Novel berberine derivatives as p300 histone acetyltransferase inhibitors in combination treatment for breast cancer.
Eur J Med Chem 266:
Sichuan University
Discovery of a novel lead characterized by a stilbene-extended scaffold against sepsis as soluble epoxide hydrolase inhibitors.
Eur J Med Chem 266:
Beijing Institute of Technology
Design, synthesis, and pharmacological evaluation of indole-piperidine amides as Blood-brain barrier permeable dual cholinesterase and β-secretase inhibitors.
Eur J Med Chem 266:
Csir-Indian Institute of Integrative Medicine
Ligand-Based Competition Binding by Real-Time
J Med Chem 67: 1115-1126 (2024)
University of Bologna
Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy.
J Med Chem 67: 922-951
Zhengzhou University
Discovery of TP0628103: A Highly Potent and Selective MMP-7 Inhibitor with Reduced OATP-Mediated Clearance Designed by Shifting Isoelectric Points.
J Med Chem 67: 1406-1420
Taisho Pharmaceutical Co., Ltd.
Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.
J Med Chem 67: 1460-1480
Stanford University
Design, synthesis and biological evaluation of 6-chloro-quinolin-2-one derivatives as novel FXIa inhibitors.
Bioorg Med Chem Lett 99:
Puchuang Pharmaceutical Technology (Tianjin) Co., Ltd
HDAC-targeting epigenetic modulators for cancer immunotherapy.
Eur J Med Chem 265:
Hubei Polytechnic University
Discovery of Novel Pyridazine-Tethered Sulfonamides as Carbonic Anhydrase II Inhibitors for the Management of Glaucoma.
J Med Chem 67: 1611-1623
Tanta University
Unraveling the Puzzle of Therapeutic Peptides: A Promising Frontier in Huntington's Disease Treatment.
J Med Chem 67: 783-815
Aligarh Muslim University
Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo.
J Med Chem 67: 1563-1579
East China University of Science and Technology
Design, synthesis, and evaluation of dual EGFR/AURKB inhibitors as anticancer agents for non-small cell lung cancer.
Bioorg Med Chem Lett 100:
Ferris State University
Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3.
Bioorg Med Chem Lett 99:
University of North Carolina at Chapel Hill
Therapeutic potential of targeting polo-like kinase 4.
Eur J Med Chem 265:
Sichuan University
RIPK1 inhibitors: A key to unlocking the potential of necroptosis in drug development.
Eur J Med Chem 265:
Lanzhou University Second Hospital
N-(Heteroaryl)thiophene sulfonamides as angiotensin AT2 receptor ligands.
Eur J Med Chem 265:
Uppsala University
The formyl peptide receptors FPR1 and FPR2 as targets for inflammatory disorders: recent advances in the development of small-molecule agonists.
Eur J Med Chem 265:
Monash University
Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders.
Eur J Med Chem 265:
Jamia Millia Islamia
Emerging Drug Targets for Antimalarial Drug Discovery: Validation and Insights into Molecular Mechanisms of Function.
J Med Chem 67: 838-863
University of Zambia
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
J Med Chem 67: 1447-1459
Novartis Institutes for Biomedical Research
Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase.
J Med Chem 67: 1061-1078 (2024)
Imperial College London
Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRASG12D.
J Med Chem 67: 1147-1167
Shanghai Institute of Materia Medica
Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.
J Med Chem 67: 864-884 (2024)
Astrazeneca
An overview of the functions of p53 and drugs acting either on wild- or mutant-type p53.
Eur J Med Chem 265:
Shandong University
Small molecule modulators of cystic fibrosis transmembrane conductance regulator (CFTR): Structure, classification, and mechanisms.
Eur J Med Chem 265:
China Pharmaceutical University
An 19F NMR fragment-based approach for the discovery and development of BRCA2-RAD51 inhibitors to pursuit synthetic lethality in combination with PARP inhibition in pancreatic cancer.
Eur J Med Chem 265:
Istituto Italiano di Tecnologia
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
J Med Chem 67: 1580-1610 (2024)
Jagiellonian University Medical College
Structure-Activity Relationships and Discovery of (S)-6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro-6H-pyrido[1,2-h][1,7]naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer.
J Med Chem 67: 1421-1446
Arbutus Biopharma
Discovery of Novel and Potent Prolyl Hydroxylase Domain-Containing Protein (PHD) Inhibitors for The Treatment of Anemia.
J Med Chem 67: 1393-1405
Insilico Medicine Shanghai Ltd
Design of cyclic peptides as novel inhibitors of ICOS/ICOSL interaction.
Bioorg Med Chem Lett 99:
Weill Cornell Medicine
Discovery of N-alkyl-N-benzyl thiazoles as novel TRPC antagonists for the treatment of glioblastoma multiforme.
Eur J Med Chem 265:
Yantai University
Targeting aromatase to restrain oestrogen production and developing efficacious interventions against ER-positive cancer.
Eur J Med Chem 265:
Guru Nanak Dev University
Benzopyran hydrazones with dual PPARα/γ or PPARα/δ agonism and an anti-inflammatory effect on human THP-1 macrophages.
Eur J Med Chem 265:
University of Valencia
Synthesis and clinical application of new drugs approved by FDA in 2023.
Eur J Med Chem 265:
First People's Hospital of Shangqiu
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Eur J Med Chem 265:
Sichuan University
Rising Star in Immunotherapy: Development and Therapeutic Potential of Small-Molecule Inhibitors Targeting Casitas B Cell Lymphoma-b (Cbl-b).
J Med Chem 67: 816-837
China Pharmaceutical University
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
J Med Chem 67: 1262-1313
Arvinas LLC
Hepatitis C: The Story of a Long Journey through First, Second, and Third Generation NS3/4A Peptidomimetic Inhibitors. What Did We Learn?
J Med Chem 67: 885-921
Ri.MED Foundation
Discovery of Natural Ah Receptor Antagonists from Salvia miltiorrhiza Bunge and Synthesis of Analogs for Tumor Immunotherapy.
J Med Chem 67: 1243-1261
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors.
J Med Chem 67: 1544-1562
Novartis Biomedical Research
Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.
J Med Chem 67: 1513-1532
China Pharmaceutical University
Development of Antibacterial Peptides with Membrane Disruption and Folate Pathway Inhibitory Activities against Methicillin-Resistant Staphylococcus aureus.
J Med Chem 67: 1044-1060
Qilu University of Technology (Shandong Academy of Sciences)
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity.
Bioorg Med Chem 98:
University of Selcuk
Ferroptosis and its modulators: A raising target for cancer and Alzheimer's disease.
Bioorg Med Chem 98:
Indian Institute of Technology (Banaras Hindu University)
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors.
Eur J Med Chem 265:
West China Hospital of Sichuan University
Design, synthesis, and biological evaluation of novel discoidin domain receptor inhibitors for the treatment of lung adenocarcinoma and pulmonary fibrosis.
Eur J Med Chem 265:
Sichuan University
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model.
Eur J Med Chem 265:
Sorbonne Universit£
Plasmodium falciparum topoisomerases: Emerging targets for anti-malarial therapy.
Eur J Med Chem 265:
University of Kashmir
Structure-Guided Design, Synthesis, and Antivirulence Assessment of Covalent Staphylococcus aureus Sortase A Inhibitors.
J Med Chem 67: 1127-1146
Nanjing University of Chinese Medicine
Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development.
J Med Chem 67: 952-970
Japan Tobacco
Structure-activity relationship study of 1,6-naphthyridinone derivatives as selective type II AXL inhibitors with potent antitumor efficacy.
Eur J Med Chem 265:
University of South China
Design, synthesis and antitumor activity of 4-arylamine substituted pyrimidine derivatives as noncovalent EGFR inhibitors overcoming C797S mutation.
Eur J Med Chem 265:
Guizhou University
Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity.
Bioorg Med Chem 98:
Osaka University
Identification of a Sonically Activated Degrader of Methionine Adenosyltransferase 2A by an in Silico Approach Assisted with the Hole-Electron Analysis.
J Med Chem 67: 543-554
Guizhou University
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.
J Med Chem 67: 1079-1092
Nanjing University of Chinese Medicine
Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist.
J Med Chem 67: 643-673
Gedeon Richter Plc
Fragment Merging, Growing, and Linking Identify New Trypanothione Reductase Inhibitors for Leishmaniasis.
J Med Chem 67: 402-419 (2024)
Sapienza University of Rome
Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles.
J Med Chem 67: 38-64
Joint Research Institution of Altitude Health and Institute of Respiratory Health and National Clinical Research Center for Geriatrics
Broad-spectrum antiviral strategy: Host-targeting antivirals against emerging and re-emerging viruses.
Eur J Med Chem 265:
Shandong University
Progress in the controllability technology of PROTAC.
Eur J Med Chem 265:
Changzhou Vocational Institute of Engineering
Target identification, and optimization of dioxygenated amide derivatives as potent antibacterial agents with FabH inhibitory activity.
Eur J Med Chem 265:
Anhui University of Chinese Medicine
Structural modification of C2-substituents on 1,4-bis(arylsulfonamido)benzene or naphthalene-N,N'-diacetic acid derivatives as potent inhibitors of the Keap1-Nrf2 protein-protein interaction.
Eur J Med Chem 265:
The State University of New Jersey
From Hit to Lead: Structure-Based Optimization of Novel Selective Inhibitors of Receptor-Interacting Protein Kinase 1 (RIPK1) for the Treatment of Inflammatory Diseases.
J Med Chem 67: 754-773
Sichuan University
A Simple Chiral
J Nat Prod 87: 77-84 (2024)
National and Kapodistrian University of Athens
Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.
Bioorg Med Chem 98:
University of Campinas
Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease.
Eur J Med Chem 265:
Shenyang Pharmaceutical University
Molecular Pharmacology Profiling of Phenylfentanil and Its Analogues to Understand the Putative Involvement of an Adrenergic Mechanism in Fentanyl-Induced Respiratory Depression.
J Med Chem 67: 603-619
Virginia Commonwealth University
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
J Med Chem 67: 774-781 (2024)
Mirati Therapeutics
Discovery of 4-Ethoxy-6-chloro-5-azaindazoles as Novel PDE4 Inhibitors for the Treatment of Alcohol Use Disorder and Alcoholic Liver Diseases.
J Med Chem 67: 728-753
Southern Medical University
Thiazol-4(5H)-one analogs as potent tyrosinase inhibitors: Synthesis, tyrosinase inhibition, antimelanogenic effect, antioxidant activity, and in silico docking simulation.
Bioorg Med Chem 98:
Pusan National University
Discovery of Novel Inhibitors of BRD4 for Treating Prostate Cancer: A Comprehensive Case Study for Considering Water Networks in Virtual Screening and Drug Design.
J Med Chem 67: 138-151
Zhejiang University
Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior.
J Med Chem 67: 529-542
University of Illinois Chicago
Coriaceumins A-D, the First Nitrogen-Containing Crenulide Diterpenoids from the Brown Alga
J Nat Prod 87: 121-131 (2024)
The Second Affiliated Hospital of Nanchang University
Resveratrol-derived inhibitors of the E3 ubiquitin ligase PELI1 inhibit the metastasis of triple-negative breast cancer.
Eur J Med Chem 265:
Shandong University
Comprehensive and critical view on the anti-inflammatory and immunomodulatory role of natural phenolic antioxidants.
Eur J Med Chem 265:
University of Agronomic Sciences and Veterinary Medicine of Bucharest
Design and Discovery of Novel NLRP3 Inhibitors and PET Imaging Radiotracers Based on a 1,2,3-Triazole-Bearing Scaffold.
J Med Chem 67: 555-571
Virginia Commonwealth University
Discovery of 2-Ethoxy-5-isobutyramido-N-1-substituted Benzamide Derivatives as Selective Kv2.1 Inhibitors with In Vivo Neuroprotective Effects.
J Med Chem 67: 213-233
Chinese Academy of Medical Sciences and Peking Union Medical College
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
J Med Chem 67: 380-401 (2024)
Galapagos
Discovery of Tetrahydropyrazolopyrazine Derivatives as Potent and Selective MYT1 Inhibitors for the Treatment of Cancer.
J Med Chem 67: 420-432
Insilico Medicine Shanghai Ltd
ω-(5-Phenyl-2H-tetrazol-2-yl)alkyl-substituted glycine amides and related compounds as inhibitors of the amine oxidase vascular adhesion protein-1 (VAP-1).
Bioorg Med Chem 98:
Monsters University
Design, synthesis, and biological evaluation of HDAC6 inhibitors targeting L1 loop and serine 531 residue.
Eur J Med Chem 265:
Keimyung University
Discovery of a brain-permeable bromodomain and extra terminal domain (BET) inhibitor with selectivity for BD1 for the treatment of multiple sclerosis.
Eur J Med Chem 265:
China Pharmaceutical University
Targeted regulated cell death with small molecule compounds in colorectal cancer: Current perspectives of targeted therapy and molecular mechanisms.
Eur J Med Chem 265:
Sichuan University
Discovery and characterization of novel TRPML1 agonists.
Bioorg Med Chem Lett 98: (2024)
Arkuda Therapeutics
Dual-targeting compounds possessing enhanced anticancer activity via microtubule disruption and histone deacetylase inhibition.
Eur J Med Chem 265:
National Taiwan University
Pyrrolopyrimidine based CSF1R inhibitors: Attempted departure from Flatland.
Eur J Med Chem 265:
Norwegian University of Science and Technology (NTNU)
Discovery of hydroxamate as a promising scaffold dually inhibiting metallo- and serine-β-lactamases.
Eur J Med Chem 265:
Northwest University
Curcumin hybrid molecules for the treatment of Alzheimer's disease: Structure and pharmacological activities.
Eur J Med Chem 265:
Ningxia Medical University
Dual target PARP1/EZH2 inhibitors inducing excessive autophagy and producing synthetic lethality for triple-negative breast cancer therapy.
Eur J Med Chem 265:
China Pharmaceutical University
DW71177: A novel [1,2,4]triazolo[4,3-a]quinoxaline-based potent and BD1-Selective BET inhibitor for the treatment of acute myeloid leukemia.
Eur J Med Chem 265:
Korea Research Institute of Chemical Technology
Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors.
J Med Chem 67: 2-16
The State University of New York
Diaporaustalides A-L, Austalide Meroterpenoids from a Plant Endophytic
J Nat Prod 87: 141-151 (2024)
Huazhong University of Science and Technology
Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.
J Med Chem 67: 322-348
China Pharmaceutical University
Sialyl LewisX glycomimetics bearing an extended anionic chain targeting E- and P- selectin binding sites.
Bioorg Med Chem 98:
University of Montreal
Discovery of a 1,6-naphthyridin-4-one-based AXL inhibitor with improved pharmacokinetics and enhanced in vivo antitumor efficacy.
Eur J Med Chem 265:
University of Chinese Academy of Sciences
Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3.
J Med Chem 67: 674-690
Goethe University Frankfurt
Smart glypican-3-targeting peptide-chlorin e6 conjugates for targeted photodynamic therapy of hepatocellular carcinoma.
Eur J Med Chem 264:
Second Military Medical University (Naval Medical University)
Target Separation and Potential Anticancer Activity of Withanolide-Based Glucose Transporter Protein 1 Inhibitors from
J Nat Prod 87: 2-13 (2024)
China Pharmaceutical University
Discovery, Optimization, and Evaluation of Potent and Selective DNA-PK Inhibitors in Combination with Chemotherapy or Radiotherapy for the Treatment of Malignancies.
J Med Chem 67: 245-271
West China Hospital
Discovery of Potent and Selective Phosphatidylinositol 3-Phosphate 5-Kinase (PIKfyve) Inhibitors as Methuosis Inducers.
J Med Chem 67: 165-179
Sichuan University/West China School of Nursing
Exploiting the Carboxylate-Binding Pocket of β-Lactamase Enzymes Using a Focused DNA-Encoded Chemical Library.
J Med Chem 67: 620-642
Baylor College of Medicine
Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile.
J Med Chem 67: 709-727
National Institute on Drug Abuse - Intramural Research Program
Lead Optimization of BIBR1591 To Improve Its Telomerase Inhibitory Activity: Design and Synthesis of Novel Four Chemical Series with In Silico, In Vitro, and In Vivo Preclinical Assessments.
J Med Chem 67: 492-512
Horus University-Egypt
Novel IRAK4 Inhibitors for Treating Asthma, COPD, Cancer, Autoinflammatory Diseases, and Autoimmune Diseases.
ACS Med Chem Lett 14: 1617-1618 (2023)
Smith, Gambrell & Russell
Discovery of 5-Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors.
ACS Med Chem Lett 14: 1673-1681 (2023)
Pfizer
Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.
ACS Med Chem Lett 14: 1848-1856 (2023)
Astrazeneca
Novel Fused Pyrazole Amide Analogs as Glucosylceramide Synthase Inhibitors for Treating Lysosomal Storage Diseases, Neurodegenerative Diseases, Cystic Diseases, and Cancer.
ACS Med Chem Lett 14: 1621-1622 (2023)
Smith, Gambrell & Russell
2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A
ACS Med Chem Lett 14: 1640-1646 (2023)
National Institute of Diabetes and Digestive and Kidney Disease
Novel Indane-Containing NBTIs with Potent Anti-Gram-Negative Activity and Minimal hERG Inhibition.
ACS Med Chem Lett 14: 1791-1799 (2023)
Roche Pharma Research & Early Development
Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors.
ACS Med Chem Lett 14: 1863-1868 (2023)
University of Bonn
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.
ACS Med Chem Lett 14: 1631-1639 (2023)
Novartis Institutes for Biomedical Research
Novel Adenosine Receptor Antagonists for Treating Cancer and Immune-Related Disorders.
ACS Med Chem Lett 14: 1619-1620 (2023)
Smith, Gambrell & Russell
Phenyl-quinoline-xxo-butyric Acid Inhibitors of Histone Lysine Demethylase for the Treatment of Cancer.
ACS Med Chem Lett 14: 1623-1624 (2023)
Arrival Discovery
Discovery of Potent and Oral Bioavailable MAT2A Inhibitors for the Treatment of MTAP-Deleted Tumors.
ACS Med Chem Lett 14: 1876-1881 (2023)
Hubei Bio-Pharmaceutical Industrial Technological Institute
Novel PARP7 Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 1615-1616 (2023)
Smith, Gambrell & Russell
Fragment-Based Screening Identifies New Quinazolinone-Based Inositol Hexakisphosphate Kinase (IP6K) Inhibitors.
ACS Med Chem Lett 14: 1760-1766 (2023)
Lieber Institute For Brain Development
Tuning the Reactivity of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Optimal
ACS Med Chem Lett 14: 1700-1706 (2023)
Rigel Pharmaceuticals
Nanomolar Benzothiazole-Based Inhibitors of 17β-HSD10 with Cellular Bioactivity.
ACS Med Chem Lett 14: 1724-1732 (2023)
University of Hradec Kralove
Discovery of Novel NLRP3 Inflammasome Inhibitors Composed of an Oxazole Scaffold Bearing an Acylsulfamide.
ACS Med Chem Lett 14: 1833-1838 (2023)
Japan Tobacco
The Promiscuity of Disulfiram in Medicinal Research.
ACS Med Chem Lett 14: 1610-1614 (2023)
Palacky University
Synthesis and Evaluation of Small Molecule Inhibitors of the Androgen Receptor N-Terminal Domain.
ACS Med Chem Lett 14: 1800-1806 (2023)
University of Strathclyde
Novel Pyrido[3,2-
ACS Med Chem Lett 14: 1627-1628 (2023)
Smith, Gambrell & Russell
Development of Allosteric NIK Ligands from Fragment-Based NMR Screening.
ACS Med Chem Lett 14: 1815-1820 (2023)
University of Minnesota
Electrophilic MiniFrags Revealed Unprecedented Binding Sites for Covalent HDAC8 Inhibitors.
J Med Chem 67: 572-585 (2024)
Hun-Ren Research Centre for Natural Sciences
Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.
J Med Chem 67: 17-37 (2024)
National Research Council of Italy
Targeted Degradation of PCSK9 In Vivo by Autophagy-Tethering Compounds.
J Med Chem 67: 433-449
Fudan University
Aurones and derivatives as promising New Delhi metallo-β-lactamase (NDM-1) inhibitors.
Bioorg Med Chem 97: (2024)
Univ. Grenoble Alpes
Discovery of Novel PD-L1 Inhibitors That Induce the Dimerization, Internalization, and Degradation of PD-L1 Based on the Fragment Coupling Strategy.
J Med Chem 66: 16807-16827 (2023)
China Pharmaceutical University
Synthesis, biological and molecular modelling for 1,3,4-thiadiazole sulfonyl thioureas: bacterial and fungal activity.
RSC Med Chem 14: 2751-2767 (2023)
Vietnam National University
Novel pyrazolo[3,4-
RSC Med Chem 14: 2640-2657 (2023)
Misr University for Science and Technology (MUST)
Naphthyl bearing 1,3,4-thiadiazoleacetamides targeting the parasitic folate pathway as anti-infectious agents:
RSC Med Chem 14: 2768-2781 (2023)
Jamia Millia Islamia
Discovery of novel tubulin CBSI
RSC Med Chem 14: 2738-2750 (2023)
Fudan University
Overview of CFTR activators and their recent studies for dry eye disease: a review.
RSC Med Chem 14: 2459-2472 (2023)
Shenyang Pharmaceutical University
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry.
RSC Med Chem 14: 2509-2534 (2023)
Mahatma Gandhi University
A covalent fragment-based strategy targeting a novel cysteine to inhibit activity of mutant EGFR kinase.
RSC Med Chem 14: 2731-2737 (2023)
Daiichi Sankyo Co.
Research status of indole-modified natural products.
RSC Med Chem 14: 2535-2563 (2023)
Yanbian University
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity.
RSC Med Chem 14: 2677-2698 (2023)
National Institute of Pharmaceutical Education and Research (NIPER)
A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response.
RSC Med Chem 14: 2625-2639 (2023)
Yunnan University
Degradation of Polo-like Kinase 1 by the Novel Poly-Arginine N-Degron Pathway PROTAC Regulates Tumor Growth in Nonsmall Cell Lung Cancer.
J Med Chem 67: 3307-3320
Korea Basic Science Institute (KBSI)
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors.
J Med Chem 66: 17044-17058 (2023)
Sichuan University
Discovery of potential scaffolds for glutaminyl cyclase inhibitors: Virtual screening, synthesis, and evaluation.
Bioorg Med Chem 97: (2024)
Shenzhen University Medical School
Design, synthesis and bioactivity evaluation of novel fusion peptides and their CPT conjugates inducing effective anti-tumor responses on HER2 positive tumors.
Eur J Med Chem 264:
China Pharmaceutical University
Linker optimization and activity validation of a cell surface vimentin targeted homo-dimeric peptoid antagonist for lung cancer stem cells.
Bioorg Med Chem 97: (2024)
University of Houston
Click chemistry-aided drug discovery: A retrospective and prospective outlook.
Eur J Med Chem 264:
Hangzhou Normal University
Discovery of pyrazolopyrimidines that selectively inhibit CSF-1R kinase by iterative design, synthesis and screening against glioblastoma cells.
RSC Med Chem 14: 2611-2624 (2023)
University of Edinburgh
Design, synthesis, and biological evaluation of novel 8-substituted quercetin derivatives targeting the β‑catenin/B-cell lymphoma 9 interaction.
Bioorg Med Chem Lett 98: (2024)
Tongji University
Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1).
Bioorg Med Chem Lett 98: (2024)
Princeton University
Novel orally bioavailable piperidine derivatives as extracellular arginase inhibitors developed by a ring expansion.
Eur J Med Chem 264:
Molecure
Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs).
J Med Chem 66: 16704-16727 (2023)
University of Arizona
One-Pot Synthesis of Cereblon Proteolysis Targeting Chimeras via Photoinduced C(sp
J Med Chem 66: 16939-16952 (2023)
Boehringer Ingelheim Rcv
Development of MPS1 Inhibitors: Recent Advances and Perspectives.
J Med Chem 66: 16484-16514 (2023)
Guizhou University
Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation.
J Med Chem 66: 16187-16200 (2023)
China Pharmaceutical University
Small Molecule Inhibitors Targeting the "Undruggable" Survivin: The Past, Present, and Future from a Medicinal Chemist's Perspective.
J Med Chem 66: 16515-16545 (2023)
University of Toledo College of Medicine and Life Sciences
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.
Bioorg Med Chem Lett 98: (2024)
Shanghai Institute of Materia Medica
Design, synthesis and evaluation of novel UDCA-aminopyrimidine hybrids as ATX inhibitors for the treatment of hepatic and pulmonary fibrosis.
Eur J Med Chem 264:
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Orally Available and Brain Penetrant AEP Inhibitors.
J Med Chem 66: 17026-17043 (2023)
Roche Innovation Center Basel
Discovery and Mechanistic Study of Novel
J Med Chem 66: 16597-16614 (2023)
Sichuan University
Optimization of the Antibacterial Spectrum and the Developability Profile of the Novel-Class Natural Product Corramycin.
J Med Chem 66: 16869-16887 (2023)
Evotec
Advances in Development of Selective Antitumor Inhibitors That Target PARP-1.
J Med Chem 66: 16464-16483 (2023)
Shandong University
Small molecular CD73 inhibitors: Recent progress and future perspectives.
Eur J Med Chem 264:
China Medical University
Discovery of potent and selective c-Met inhibitors for MET-amplified hepatocellular carcinoma treatment.
Eur J Med Chem 264:
China Pharmaceutical University
Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors.
J Med Chem 66: 16783-16806 (2023)
Institute of Chemical Biology
Design and Development of IKZF2 and CK1α Dual Degraders.
J Med Chem 66: 16953-16979 (2023)
Harvard University
Optimization of Pharmacokinetic and In Vitro Safety Profile of a Series of Pyridine Diamide Indirect AMPK Activators.
J Med Chem 66: 17086-17104 (2023)
Rigel Pharmaceuticals
Pioneering 4,11-Dioxo-4,11-dihydro-1
J Med Chem 66: 16843-16868 (2023)
Shanghai Jiao Tong University
Investigating the anti-cancer potential of pyrimethamine analogues through a modern chemical biology lens.
Eur J Med Chem 264:
University of British Columbia
Targeting PIM kinases in cancer therapy: An update on pharmacological small-molecule inhibitors.
Eur J Med Chem 264:
Sichuan University
Design and synthesis of dual BRD4/Src inhibitors for treatment of triple-negative breast cancer.
Eur J Med Chem 264:
Shenzhen University
Discovery and biological evaluation of novel dual PTP1B and ACP1 inhibitors for the treatment of insulin resistance.
Bioorg Med Chem 97: (2024)
The Affiliated Hospital of Yangzhou University
Design, synthesis and anti-rheumatoid arthritis activity of target TLR4 inhibitors.
Bioorg Med Chem 97: (2024)
Chongqing Chemical Industry Vocational College
Discovery of flavone-derivatives as the new skeleton of transient receptor potential vanilloid 3 channel antagonists.
Bioorg Med Chem Lett 98: (2024)
Qingdao University Medical College
Synthesis, activity, and their relationships of 2,4-diaminonicotinamide derivatives as EGFR inhibitors targeting C797S mutation.
Bioorg Med Chem Lett 98: (2024)
Daiichi Sankyo Co.
Structure-based design of SARS-CoV-2 papain-like protease inhibitors.
Eur J Med Chem 264:
State University of New Jersey
Structural Fusion of Natural and Synthetic Ligand Features Boosts RXR Agonist Potency.
J Med Chem 66: 16762-16771 (2023)
Goethe University Frankfurt
Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
J Med Chem 66: 16991-17025 (2023)
Shanghai Institute of Materia Medica
Identification of a novel potent CDK inhibitor degrading cyclinK with a superb activity to reverse trastuzumab-resistance in HER2-positive breast cancer in vivo.
Eur J Med Chem 264:
Hanyang University
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism.
Eur J Med Chem 264:
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Dual Function Agents That Exhibit Anticancer Activity via Catastrophic Nicotinamide Adenine Dinucleotide Depletion.
J Med Chem 66: 16694-16703 (2023)
Nanchang University
Discovery of YSR734: A Covalent HDAC Inhibitor with Cellular Activity in Acute Myeloid Leukemia and Duchenne Muscular Dystrophy.
J Med Chem 66: 16658-16679 (2023)
University of Toronto Mississauga
Discovery of Highly Selective PARP7 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
J Med Chem 67: 1932-1948
China Pharmaceutical University
Discovery of Selective and Orally Available Galectin-1 Inhibitors.
J Med Chem 66: 16980-16990 (2023)
Galecto Biotech
Bifunctional backbone modified squaramide dipeptides as amyloid beta (Aβ) aggregation inhibitors.
Bioorg Med Chem 97: (2024)
National Institute of Pharmaceutical Education and Research (NIPER)-Ahmedabad
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 2.
Eur J Med Chem 264:
Zhengzhou University
An imidazo[1,2-a]pyridine-pyridine derivative potently inhibits FLT3-ITD and FLT3-ITD secondary mutants, including gilteritinib-resistant FLT3-ITD/F691L.
Eur J Med Chem 264:
University of Arkansas
Targeting the pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis to discover potent PDK inhibitors through structure-based virtual screening and pharmacological evaluation.
Eur J Med Chem 264:
Chongqing Medical and Pharmaceutical College
Is it still worth renewing nucleoside anticancer drugs nowadays?
Eur J Med Chem 264:
Jilin University
Small molecules targeting selected histone methyltransferases (HMTs) for cancer treatment: Current progress and novel strategies.
Eur J Med Chem 264:
First Affiliated Hospital of Gannan Medical University
Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer.
J Med Chem 66: 16917-16938 (2023)
East China Normal University
Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid Modulators.
J Med Chem 66: 16303-16329 (2023)
Shandong University
Design, synthesis, biological evaluation and molecular docking of alkoxyaurones as potent pancreatic lipase inhibitors.
Bioorg Med Chem Lett 98: (2024)
University of Medicine and Pharmacy At Ho Chi Minh City
PSMA-targeted small-molecule drug-conjugates with valine-citrulline and phosphoramidate cleavable linkers.
Bioorg Med Chem Lett 98: (2024)
Washington State University
Discovery of novel deoxyvasicinone derivatives with benzenesulfonamide substituents as multifunctional agents against Alzheimer's disease.
Eur J Med Chem 264:
Anhui Medical University
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
J Med Chem 66: 15648-15670 (2023)
Perha Pharmaceuticals
Harnessing the Reactivity of Duclauxin toward Obtaining
J Med Chem 66: 16222-16234 (2023)
National Autonomous University of Mexico
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia.
Eur J Med Chem 264:
Chinese Academy of Medical Sciences & Peking Union Medical College
Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus infection.
Eur J Med Chem 264:
Shaanxi University of Science & Technology
Small Molecule Ligands of the BET-like Bromodomain,
J Med Chem 66: 15801-15822 (2023)
University of Oxford
Discovery of a First-in-Class GPR183 Antagonist for the Potential Treatment of Rheumatoid Arthritis.
J Med Chem 66: 15926-15943 (2023)
TBA
Discovery of 4-aminophenylacetamide derivatives as intestine-specific farnesoid X receptor antagonists for the potential treatment of nonalcoholic steatohepatitis.
Eur J Med Chem 264:
Guilin Medical University
Recent progress and applications of small molecule inhibitors of Keap1-Nrf2 axis for neurodegenerative diseases.
Eur J Med Chem 264:
Hangzhou City University
The discovery of aryl-2-nitroethyl triamino pyrimidines as anti-Trypanosoma brucei agents.
Eur J Med Chem 264:
University of Modena and Reggio Emilia
Structure-based design of potent FABP4 inhibitors with high selectivity against FABP3.
Eur J Med Chem 264:
University of Chinese Academy of Sciences
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment.
Eur J Med Chem 264:
First Affiliated Hospital of Gannan Medical University
Benzothiozinone derivatives with anti-tubercular Activity-Further side chain investigation.
Eur J Med Chem 264:
Suzhou Medical College of Soochow University
Design and synthesis of the first PARP-1 and proteasome dual inhibitors to treat breast cancer.
Eur J Med Chem 264:
Sichuan University
Synthetic GPR40/FFAR1 agonists: An exhaustive survey on the most recent chemical classes and their structure-activity relationships.
Eur J Med Chem 264:
Jadavpur University
Blood-stage antimalarial activity, favourable metabolic stability and in vivo toxicity of novel piperazine linked 7-chloroquinoline-triazole conjugates.
Eur J Med Chem 264:
Jawaharlal Nehru University
Discovery of Inhibitory Fragments That Selectively Target Spire2-FMN2 Interaction.
J Med Chem 66: 15715-15727 (2023)
Jagiellonian University
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase.
Bioorg Med Chem Lett 98: (2024)
University of Cambridge
Biological evaluation of indolactams for in vitro bryostatin 1-like activity.
Bioorg Med Chem Lett 97:
California State University Fullerton
Discovery of Potent, Selective, and Orally Bioavailable DYRK2 Inhibitors for the Treatment of Prostate Cancer.
J Med Chem 66: 16235-16256 (2023)
China Pharmaceutical University
Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.
J Med Chem 66: 16342-16363 (2023)
Ewha Womans University
Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance.
Eur J Med Chem 264:
Shenyang Pharmaceutical University
Synthesis and biological evaluation of indole derivatives containing thiazolidine-2,4-dione as α-glucosidase inhibitors with antidiabetic activity.
Eur J Med Chem 264:
Wuyi University
Discovery of Novel 2,3-Dihydro-1
J Med Chem 66: 16141-16167 (2023)
Ocean University of China
α-Aminophosphonate inhibitors of metallo-β-lactamases NDM-1 and VIM-2.
RSC Med Chem 14: 2277-2300 (2023)
Uppsala University
Novel styryl-thiazole hybrids as potential anti-Alzheimer's agents.
RSC Med Chem 14: 2315-2326 (2023)
University of Athens
Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer.
J Med Chem 66: 16168-16186 (2023)
Icahn School of Medicine At Mount Sinai
Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes.
Eur J Med Chem 264:
Purdue University
A Novel Bifunctional μOR Agonist and σ
J Med Chem 66: 16257-16275 (2023)
Sichuan University
Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase.
J Med Chem 66: 16410-16425 (2023)
Novartis Pharma
Orthogonal Reversed-Phase C
J Nat Prod 86: 2638-2650 (2023)
University of Copenhagen
Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2).
J Med Chem 66: 15750-15760 (2023)
Bristol Myers Squibb
Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3.
Bioorg Med Chem Lett 97:
Cedars-Sinai Medical Center
Design, synthesis and evaluation of novel thieno[2,3d]pyrimidine derivatives as potent and specific RIPK2 inhibitors.
Bioorg Med Chem Lett 97:
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Synthesis, in vitro Α-Glucosidase, and acetylcholinesterase inhibitory activities of novel Indol-Fused Pyrano[2,3-D]Pyrimidine compounds.
Bioorg Med Chem Lett 98: (2024)
Vietnam Academy of Science and Technology
A novel scaffold long-acting selective estrogen receptor antagonist and degrader with superior preclinical profile against ER+ breast cancer.
Eur J Med Chem 264:
Yantai University
Discovery of conformationally constrained c-Abl inhibitors with potential neuroprotective effects against Parkinson's disease.
Bioorg Med Chem 96: (2023)
Southern Medical University
The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers.
Bioorg Med Chem Lett 97:
Zhengzhou University
Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7.
Eur J Med Chem 263:
Tianjin University
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