132 articles for X Ma
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Article Title
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Design, Synthesis, and Biological Evaluation of Coupled Bioactive Scaffolds as Potential Anticancer Agents for Dual Targeting of Dihydrofolate Reductase and Thioredoxin Reductase.
National University of Singapore
Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.
Purdue University
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.
Hangzhou Xixi Hospital
Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
Dalian Medical University
Design, synthesis, docking studies and biological evaluation of novel dihydro-1,3,5-triazines as human DHFR inhibitors.
Shanghai Institute of Pharmaceutical Industry
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.
Global Blood Therapeutics
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
Dalian Medical University
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
Dalian Medical University
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.
Clinical Research Institute of Montreal
Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors.
Dalian Medical University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
Zhejiang University
Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists.
Peking University
Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.
Dalian Medical University
Straightforward and effective synthesis of¿-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes.
University of Louvain
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.
Novartis Institutes For Biomedical Research
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.
Xuanzhu Pharma
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
Involvement of organic anion-transporting polypeptides in the hepatic uptake of dioscin in rats and humans.
Dalian Medical University
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.
Zhejiang University
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.
Zhejiang University
Synthesis and bioevaluation of 2-phenyl-4-methyl-1,3-selenazole-5-carboxylic acids as potent xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.
Zhejiang University
Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia.
Zhejiang University
Discovery of N-substituted oseltamivir derivatives as potent and selective inhibitors of H5N1 influenza neuraminidase.
Shandong University
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
China Pharmaceutical University
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Genentech
Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Genentech
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.
Zhejiang University
Antifolate and antiproliferative activity of 6,8,10-triazaspiro[4.5]deca-6,8-dienes and 1,3,5-triazaspiro[5.5]undeca-1,3-dienes.
National University of Singapore
Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers.
National University of Singapore
Synthesis and antimicrobial activity of N¹-benzyl or N¹-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines.
Huazhong University of Science and Technology
Metabolism-guided development of Ko143 analogs as ABCG2 inhibitors.
University of Pittsburgh
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.
Ocean University of China
Small Molecules Blocking the Assembly of TCAB1 and Telomerase Complexes: Lead Discovery and Biological Activity.
Anhui University of Chinese Medicine
Recent progress in the development of hypoxia-inducible factor 2α (HIF-2α) modulators: Inhibitors, agonists, and degraders (2009-2024).
Hubei Polytechnic University
Identification of naphthalimide-derivatives as novel PBD-targeted polo-like kinase 1 inhibitors with efficacy in drug-resistant lung cancer cells.
Guangxi Normal University
Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo[4,5-c]quinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation.
Sichuan University
Design, Synthesis, and Biological Evaluation of Pierardine Derivatives as Novel Brain-Penetrant and In Vivo Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
Anhui University of Chinese Medicine
A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRASG12C Inhibitor.
Ocean University of China
Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor.
Nanjing University of Chinese Medicine
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
Shanghai Institute of Materia Medica
Discovery of Novel Proteolysis-Targeting Chimera Molecules as Degraders of Programmed Cell Death-Ligand 1 for Breast Cancer Therapy.
Sichuan University
Discovery and development of palmatine analogues as anti-NASH agents by activating farnesoid X receptor (FXR).
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of novel hybrids of mTOR inhibitor and NO donor as potential anti-tumor therapeutics.
Anhui University of Chinese Medicine
Exploitation of Proximity-Mediated Effects in Drug Discovery: An Update of Recent Research Highlights in Perturbing Pathogenic Proteins and Correlated Issues.
Anhui University of Chinese Medicine
Discovery of N-substituted oseltamivir derivatives as novel neuraminidase inhibitors with improved drug resistance profiles and favorable drug-like properties.
Shandong University
Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia.
Anhui Medical University
Discovery of the GSH responsive "Y-PROTACs" targeting ALK and CDK4/6 as a potential treatment for cancer.
West China Hospital of Sichuan University
Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups--new classes of PPAR gamma/delta and PPAR alpha/gamma/delta agonists.
Bayer Pharmaceuticals
Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors.
East China University of Science and Technology
Synthesis and biological evaluation of N-(benzene sulfonyl)acetamide derivatives as anti-inflammatory and analgesic agents with COX-2/5-LOX/TRPV1 multifunctional inhibitory activity.
Anhui University of Chinese Medicine
Identification of a Novel Potent CYP4Z1 Inhibitor Attenuating the Stemness of Breast Cancer Cells through Lead Optimization.
China Pharmaceutical University
Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
Anhui University of Chinese Medicine
Recent advances in combretastatin A-4 codrugs for cancer therapy.
Xinxiang Medical University
Discovery of Pentacyclic Triterpenoid PROTACs as a Class of Effective Hemagglutinin Protein Degraders.
Peking University
Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis.
East China Normal University
Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer.
West China Hospital of Sichuan University
Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists.
National and Kapodistrian University of Athens
Iterative Optimization and Structure-Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors
Shandong University
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.
Chinese Academy of Sciences
Synthesis and biological evaluation of a tumor-selective degrader of PARP1.
West China Hospital of Sichuan University
Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
Anhui University of Chinese Medicine
Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.
Dalian Medical University
A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors.
Zhengzhou University
Design, synthesis, and biological evaluation of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines as potent EGFR
Shenyang Pharmaceutical University
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1
Bristol Myers Squibb
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.
Chinese Academy of Sciences
Noncovalent EGFR T790M/L858R inhibitors based on diphenylpyrimidine scaffold: Design, synthesis, and bioactivity evaluation for the treatment of NSCLC.
Dalian Medical University
Talaromynoids A-I, Highly Oxygenated Meroterpenoids from the Marine-Derived Fungus
Chinese Academy of Sciences
Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis.
Dalian Medical University
Discovery of novel N-sulfonamide-tetrahydroisoquinolines as potent retinoic acid receptor-related orphan receptor γt agonists.
Fudan University
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.
Sichuan University
Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.
University of Texas Medical Branch
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.
China Pharmaceutical University
Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
Anhui University of Chinese Medicine
The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).
Lilly Research Laboratories
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Merck And
Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases.
Fudan University
Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.
Weill Cornell Medicine
Flavonoids with Inhibitory Effects on NLRP3 Inflammasome Activation from
Sichuan University
Structurally novel PI3Kδ/γ dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation.
Anhui University of Chinese Medicine
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.
East China University of Science & Technology
Design and synthesis of potent PAR-1 antagonists based on vorapaxar.
Hebei University of Technology
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.
Dalian Medical University
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.
Dalian Medical University
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
Chinese Academy of Sciences
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor α.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.
Zhejiang University
The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC.
Shenyang Pharmaceutical University
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.
Zhejiang University
Design, synthesis and biological evaluation of "Multi-Site"-binding influenza virus neuraminidase inhibitors.
Shandong University
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
Peking Union Medical College
Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells.
The First Affiliated Hospital of Dalian Medical University
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.
East China University of Science & Technology
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.
Zhejiang University
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
Ocean University of China
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
Shandong University
Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents.
Dalian Medical University
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC).
Dalian Medical University
Discovery of traditional Chinese medicine monomers and their synthetic intermediates, analogs or derivatives for battling P-gp-mediated multi-drug resistance.
Anhui University of Chinese Medicine
Exploiting polypharmacology for improving therapeutic outcome of kinase inhibitors (KIs): An update of recent medicinal chemistry efforts.
Anhui University of Chinese Medicine
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
The First Affiliated Hospital of Dalian Medical University
Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.
Dalian Medical University
Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines.
Dalian Medical University
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
Shandong University
Design, synthesis and biological evaluation of sulfonamide-substituted diphenylpyrimidine derivatives (Sul-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with antitumor activity.
Dalian Medical University
Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
Dalian Medical University
Original endomorphin-1 analogues exhibit good analgesic effects with minimal implications for human sperm motility.
The Reproductive Medicine Special Hospital of The First Hospital of Lanzhou University
Discovery, Development, and Cellular Delivery of Potent and Selective Bicyclic Peptide Inhibitors of Grb7 Cancer Target.
Monash University
Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.
Eli Lilly
C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFR
Dalian Medical University
Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors.
Xihua University
METHOD FOR GENERATION OF CHEMICAL DERIVATIVES AGAINST TARGET PROTEIN TO BUILD AI DRUG PLATFORM
Syntekabio
Substituted benzyl-triazole compounds for Cbl-b inhibition, and further uses thereof
Nurix Therapeutics
HIF-1α inhibitor, preparation method therefor, and pharmaceutical composition for preventing or treating angiogenesis-associated eye disease, containing same as active ingredient
Seoul National University
Phosphorylated hydroxyethylamines as novel inhibitors of the bacterial cell wall biosynthesis enzymes MurC to MurF.
University of Ljubljana
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.
Nih
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.
Astrazeneca