194 articles for Y Jiang
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Article Title
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GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved
Genentech
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
Tsinghua University
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Genentech
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.
Glaxosmithkline
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
Pharmaron-Beijing
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Merck Research Laboratories
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
Shenyang Pharmaceutical University
Discovery of bis-aryl urea derivatives as potent and selective Limk inhibitors: Exploring Limk1 activity and Limk1/ROCK2 selectivity through a combined computational study.
Shanghai Institute of Technology
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
Pfizer
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
Fujian University of Traditional Chinese Medicine
Discovery of potent and selective urea-based ROCK inhibitors: Exploring the inhibitor's potency and ROCK2/PKA selectivity by 3D-QSAR, molecular docking and molecular dynamics simulations.
Shanghai Institute of Technology
Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
Shandong University
Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors.
Second Military Medical University
Design, synthesis and preliminary evaluation ofa-sulfonyl¿-(glycinyl-amino)proline peptidomimetics as matrix metalloproteinase inhibitors.
Shandong University
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
Shandong University
cis-1-Oxo-heterocyclyl-4-amido cyclohexane derivatives as NPY5 receptor antagonists.
Lundbeck Research Usa
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
Merck Research Laboratories
Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.
Merck Research Laboratories
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
Pfizer
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
TBA
Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.
Merck Research Laboratories
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
Zhejiang University
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.
Merck Research Laboratories
Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists.
Lundbeck Research Usa
Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors.
Tsinghua University
Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors.
Tsinghua University
II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.
Ligand Pharmaceuticals
Triterpene saponins from Clematis chinensis and their potential anti-inflammatory activity.
Peking University Health Science Center
3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
China Pharmaceutical University
AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo.
Shanghai Institute of Materia Medica
Design, synthesis, and biological evaluation of novel HDAC/CD13 dual inhibitors for the treatment of cancer.
Ocean University of China
Discovery of novel nucleoside derivatives as selective lysine acetyltransferase p300 inhibitors for cancer therapy.
Changsha Medical University
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia.
Ocean University of China
Discovery of Covalent MLKL PROTAC Degraders via Optimization of a Theophylline Derivative Ligand for Treating Necroptosis.
China Pharmaceutical University
Identification of an m6A Natural Inhibitor, Lobeline, That Reverses Lenvatinib Resistance in Hepatocellular Tumors.
The First Hospital of China Medical University
Psammaplin A analogues with modified disulfide bond targeting histone deacetylases: Synthesis and biological evaluation.
Ocean University of China
The U.S. FDA approved cardiovascular drugs from 2011 to 2023: A medicinal chemistry perspective.
Sichuan University
Benzodioxane Carboxamide Derivatives As Novel Monoamine Oxidase B Inhibitors with Antineuroinflammatory Activity.
Zunyi Medical University
Bipyridine Derivatives as NOP2/Sun RNA Methyltransferase 3 Inhibitors for the Treatment of Colorectal Cancer.
Zhejiang University
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
China Pharmaceutical University
Advanced Design, Synthesis, and Evaluation of Highly Selective Wee1 Inhibitors: Enhancing Pharmacokinetics and Antitumor Efficacy.
China Pharmaceutical University
HDAC/NAMPT dual inhibitors overcome initial drug-resistance in p53-null leukemia cells.
Ocean University of China
Facilitating the development of molecular glues: Opportunities from serendipity and rational design.
Sichuan University
Exploration of novel isoxazole-fused quinone derivatives as anti-colorectal cancer agents through inhibiting STAT3 and elevating ROS level.
Sichuan University
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Lundbeck Research Usa
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Lundbeck Research Usa
Strategies for the Discovery of Oxazolidinone Antibacterial Agents: Development and Future Perspectives.
Sichuan University
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery.
Shandong University
Design, synthesis and biological evaluation of 2,4,6- trisubstituted triazine derivatives as new nonpeptide small-molecule SIRT5 inhibitors.
Xihua University
Novel Sulfonylurea-Based NLRP3 Inflammasome Inhibitor for Efficient Treatment of Nonalcoholic Steatohepatitis, Endotoxic Shock, and Colitis.
Ocean University of China
Design, synthesis and biological evaluation of pyrimidine base hydroxamic acid derivatives as dual JMJD3 and HDAC inhibitors.
Tsinghua University
Structure-Activity Relationship Studies of 2,4,5-Trisubstituted Pyrimidine Derivatives Leading to the Identification of a Novel and Potent Sirtuin 5 Inhibitor against Sepsis-Associated Acute Kidney Injury.
Xihua University
Discovery of N-substituted oseltamivir derivatives as novel neuraminidase inhibitors with improved drug resistance profiles and favorable drug-like properties.
Shandong University
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.
China Pharmaceutical University
Discovery of IACS-52825, a Potent and Selective DLK Inhibitor for Treatment of Chemotherapy-Induced Peripheral Neuropathy.
The University of Texas Md Anderson Cancer Center
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Nankai University
Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations.
Jiangnan University
Selective Inhibition of PTP1B by New Anthraquinone Glycosides from
Binzhou Medical University
Discovery of Small Molecules Simultaneously Targeting NAD(P)H:Quinone Oxidoreductase 1 and Nicotinamide Phosphoribosyltransferase: Treatment of Drug-Resistant Non-small-Cell Lung Cancer.
China Pharmaceutical University
Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis.
China Pharmaceutical University
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
China Pharmaceutical University
Discovery of Novel Orally Bioavailable Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo.
Tongji University
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
Chinese Academy of Sciences
Quinazoline-based hydroxamic acid derivatives as dual histone methylation and deacetylation inhibitors for potential anticancer agents.
Tsinghua University
Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
Ocean University of China
Design, synthesis and antitumor evaluation of novel 1H-indole-2-carboxylic acid derivatives targeting 14-3-3η protein.
Tsinghua University
Exploration and Biological Evaluation of Bispecific Peptides Derived from Anti-HER2 Antibodies and Peptide-Camptothecin Conjugates for HER2-Positive Breast Cancer.
China Pharmaceutical University
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Potent Hydrazide-Based HDAC Inhibitors with a Superior Pharmacokinetic Profile for Efficient Treatment of Acute Myeloid Leukemia In Vivo.
Ocean University of China
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists.
Tsinghua University
Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings.
Emory University
Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase.
Henan Normal University
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
University of Texas
Concise solid-phase synthesis enables derivatisation of YEATS domain cyclopeptide inhibitors for improved cellular uptake.
The University of Hong Kong
Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- and BCRP-Mediated Multidrug Resistance.
China Pharmaceutical University
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR
Zhengzhou University
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
Tsinghua University
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
University of Texas Md Anderson Cancer Center
Discovery of a novel chimeric ubenimex-gemcitabine with potent oral antitumor activity.
Shandong University
Discovery of BC-01, a novel mutual prodrug (hybrid drug) of ubenimex and fluorouracil as anticancer agent.
Shandong University
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.
Southern Medical University
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
The Schering Plough Research Institute
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Astrazeneca
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.
The University of Texas Md Anderson Cancer Center
Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.
Lilly China Research and Development Center (Lcrdc)
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.
Shenyang Pharmaceutical University
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Genentech
Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.
TBA
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
Emory University School of Medicine
Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma.
Chinese Academy of Sciences
Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors.
Southern Medical University
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
Ocean University of China
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Genentech
Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.
Array Biopharma
Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.
Central South University
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Shandong 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 furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Shandong University
Structural Insights of Benzenesulfonamide Analogues as NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.
TBA
Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1.
Chongqing Medical University
Terpenoids with vasorelaxant effects from the Chinese liverwort Scapania carinthiaca.
Shandong University
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
Tsinghua University
Design, synthesis and structure-activity relationship of a focused library of β-phenylalanine derivatives as novel eEF2K inhibitors with apoptosis-inducing mechanisms in breast cancer.
Sichuan University
Discovery of 1-(3-aryl-4-chlorophenyl)-3-(p-aryl)urea derivatives against breast cancer by inhibiting PI3K/Akt/mTOR and Hedgehog signalings.
Tsinghua University
Synthesis and biological characterization of ubenimex-fluorouracil conjugates for anti-cancer therapy.
Shandong University
Design, synthesis and structure-activity relationship studies of a focused library of pyrimidine moiety with anti-proliferative and anti-metastasis activities in triple negative breast cancer.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy.
Tsinghua University
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
Genentech
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
Tsinghua University
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
East China University of Science & Technology
Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design.
Second Military Medical University
Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
Tsinghua University
Structural Biology-Inspired Discovery of Novel KRAS-PDEδ Inhibitors.
Second Military Medical University
Structural Basis of Inhibition of ERα-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.
Shenzhen Graduate School of Peking University
Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
Shandong University
SMALL MOLECULE INHIBITORS OF NAV1.8 SODIUM CHANNELS FOR PAIN RELIEF
Humanwell Pharmaceutical US
7H-PYRROLO[2,3-D]PYRIMIDINES AND PREPARATION AND USES THEREOF
Biosplice Therapeutics
Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
Prelude Therapeutics
Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors
Xenon Pharmaceuticals
An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.
University of Bonn
Inhibitor of the mutated isocitrate dehydrogenase IDH1 R132H
Bayer Pharma Aktiengesellschaft
Pyrrole six-membered heteroaryl ring derivative, preparation method thereof, and medicinal uses thereof
Jiangsu Hengrui Medicine
Cyclopentylbenzamide derivatives and their use for the treatment of psychotic and cognitive disorders
Takeda Pharmaceutical
Selective histone deactylase 6 inhibitors
H. Lee Moffitt Cancer Center and Research Institute
Biphenyl-ethyl-pyrrolidine derivatives as histamine H3 receptor modulators for the treatment of cognitive disorders
Arena Pharmaceuticals
Synthesis of a novel series of L-isoserine derivatives as aminopeptidase N inhibitors.
Shandong University
Compounds having activating effect on subtypes of peroxisome proliferator-activated receptors and its preparation method and uses
Zhejiang Hisun Pharmaceutical
Pyrazole and imidazole derivatives useful as orexin antagonists
Actelion Pharmaceuticals
6-thio-substituted imidazo[1,2-a]pyrazines as Mps-1 inhibitors
Bayer Intellectual Property
2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
Merck Sharp & Dohme
Methods and compositions for studying, imaging, and treating pain
The Leland Stanford Junior University
Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.
Icahn School Of Medicine At Mount Sinai
Development of Potent and Selective Tissue Transglutaminase Inhibitors: Their Effect on TG2 Function and Application in Pathological Conditions.
Aston University
Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pryimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea
Vertex Pharmaceuticals
4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics
Galderma Research & Development
Discovery of novel tricyclic pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amine derivatives as VEGFR-2 inhibitors.
Suez Canal University
Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as cFMS inhibitors
Array Biopharma
Discovery and Structure Optimization of a Series of Isatin Derivatives as Mycobacterium tuberculosis Chorismate Mutase Inhibitors.
Birla Institute of Technology
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells.
Nagoya University School of Medicine
Combined X-ray, NMR, and kinetic analyses reveal uncommon binding characteristics of the hepatitis C virus NS3-NS4A protease inhibitor BI 201335.
Boehringer Ingelheim (Canada)
Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Novartis Pharma
SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.
Ariad Pharmaceuticals
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.
Vanderbilt University