168 articles for W Chen
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Article Title
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Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Arena Pharmaceuticals
Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors.
Shanghaitech University
6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR.
Zhejiang University
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
Shanghai Institute of Materia Medica
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
Shandong University
Identification of benzothiophene amides as potent inhibitors of human nicotinamide phosphoribosyltransferase.
Second Military Medical University
Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: introduction of an additional carboxyl group at the C-2 position of quinoline.
China Pharmaceutical University
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
Fujian University of Traditional Chinese Medicine
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
Roche Innovation Center Shanghai
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
Shandong University
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
Shandong University
Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.
Fudan University
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
Shandong University
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Arena Pharmaceuticals
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Arena Pharmaceuticals
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors.
Chinese Academy of Sciences
Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
Shandong University
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
Shandong University
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
China Pharmaceutical University
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization.
Chinese Academy of Sciences
Thermodynamic and structural characterization of halogen bonding in protein-ligand interactions: a case study of PDE5 and its inhibitors.
Chinese Academy of Sciences (Cas)
Identification of novel HSP90a/ß isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Vertex Pharmaceuticals
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.
Zhejiang University
Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
The Scripps Research Institute
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.
Chinese Academy of Sciences
1-(4-Phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanones as novel CCR1 antagonists.
Chemocentryx
Cyanobacterial peptides as a prototype for the design of potentß-secretase inhibitors and the development of selective chemical probes for other aspartic proteases.
University of Florida
Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor.
TBA
Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.
Duke University Medical Center
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
Institute of Pharmacology and Toxicology
Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.
Translational Research Institute
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.
Millennium Pharmaceuticals
Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids.
The Hebrew University of Jerusalem
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.
The Scripps Research Institute
The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.
Merck Research Laboratories
Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.
The Scripps Research Institute
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Synthesis and antiproliferative activity of indolizine derivatives incorporating a cyclopropylcarbonyl group against Hep-G2 cancer cell line.
Nanjing University
Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.
Arena Pharmaceuticals
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.
Translational Research Institute and Department of Molecular Therapeutics
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.
Merck Research Laboratories
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
Chinese Academy of Sciences
Design and synthesis of 7-membered lactam fused hydroxypyridinones as potent metal binding pharmacophores (MBPs) for inhibiting influenza virus PAN endonuclease.
Zhejiang University
Rational Design of a Novel 6H-Benzo[c]chromen Series as Selective PI3Kα Inhibitors.
Xi'an Jiaotong University
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.
Institute of Science and Technology
Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3.
Cedars-Sinai Medical Center
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.
Scripps Florida
Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors.
China Pharmaceutical University
Discovery of matrix metalloproteinase inhibitors as anti-skin photoaging agents.
Hangzhou Normal University
Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound.
Hangzhou Normal University
Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit.
Zhejiang University
Aza analogues of equol: novel ligands for estrogen receptor beta.
Chinese Academy of Sciences
Discovery of Potent, Selective, and Orally Bioavailable DYRK2 Inhibitors for the Treatment of Prostate Cancer.
China Pharmaceutical University
Ligand-Directed Photodegradation of Interacting Proteins: Oxidative HER2/HER3 Heterodimer Degradation with a Lapatinib-Derived Photosensitizer.
Shandong University
Design, Synthesis, and Biological Evaluation of New 1H-Imidazole-2-Carboxylic Acid Derivatives as Metallo-β-Lactamase Inhibitors.
Xihua University
Discovery of Potent and Wild-Type-Sparing Fourth-Generation EGFR Inhibitors for Treatment of Osimertinib-Resistance NSCLC.
China Pharmaceutical University
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Nanjing Medical University
Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.
Millennium Pharmaceuticals
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2-p53 Inhibitor.
Unnatural Products
Discovery of Potent DYRK2 Inhibitors with High Selectivity, Great Solubility, and Excellent Safety Properties for the Treatment of Prostate Cancer.
China Pharmaceutical University
Discovery of aromatic 2-(3-(methylcarbamoyl) guanidino)-N-aylacetamides as highly potent chitinase inhibitors.
China Agricultural University
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
Therapeutic potential of targeting SHP2 in human developmental disorders and cancers.
Zhejiang University
Novel strategies to improve tumour therapy by targeting the proteins MCT1, MCT4 and LAT1.
Guang Xi University of Chinese Medicine
The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.
Merck Research Laboratories
A review on the treatment of multiple myeloma with small molecular agents in the past five years.
Sichuan Academy of Medical Science&Sichuan Provincial People'S Hospital
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.
Merck Research Laboratories
Ethers of 3-hydroxyphenylacetic acid as selective gamma-hydroxybutyric acid receptor ligands.
University of Maryland
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor.
Merck Research Laboratories
New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.
University Shihezi
Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer.
China Pharmaceutical University
Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma.
China Pharmaceutical University
Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia.
China Pharmaceutical University
Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
Shandong University
Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.
China Pharmaceutical University
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.
University of Tromsø
Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors.
Peking University
Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.
University of Texas Medical Branch
Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.
University of Michigan
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR
Zhejiang University
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1
Chinese Academy of Sciences
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
South China Agricultural University
Multitarget-directed oxoisoaporphine derivatives: Anti-acetylcholinesterase, anti-β-amyloid aggregation and enhanced autophagy activity against Alzheimer's disease.
Guangxi Normal University
Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.
University of Hawaii Cancer Center
Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation.
Hunan Agricultural University
Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.
F. Hoffmann-La Roche
Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
TBA
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.
Roche Innovation Center Shanghai
Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants.
Zhejiang University
Optimization and anti-inflammatory evaluation of methyl gallate derivatives as a myeloid differentiation protein 2 inhibitor.
Wenzhou Medical University
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.
Cadus Pharmaceutical
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Shanghai Institute of Materia Medica
Discovery of Potent, Selective, and Direct Acid Sphingomyelinase Inhibitors with Antidepressant Activity.
China Pharmaceutical University
Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.
Shandong University
Assessment of quinazolinone derivatives as novel non-nucleoside hepatitis B virus inhibitors.
Xuzhou Medical University
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.
Hutchison Medipharma
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Novartis Institutes For Biomedical Research
Modification of the Thioglycosyl-Naphthalimides as Potent and Selective Human O-GlcNAcase Inhibitors.
China Agricultural University
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
Smithkline Beecham Pharmaceuticals
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
Shandong University
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.
Medichem Research
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Novartis Institutes For Biomedical Research
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
Shandong University
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
Shandong University
Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.
Shandong University
Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors.
China Pharmaceutical University
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
Chinese Academy of Sciences
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
Shandong University
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
Shandong University
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
Shandong University
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
South China Agricultural University
Selective inhibition of β-N-acetylhexosaminidases by thioglycosyl-naphthalimide hybrid molecules.
Dalian University of Technology
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
East China University of Science and Technology
Design, synthesis and evaluation of novel phenyl propionamide derivatives as non-nucleoside hepatitis B virus inhibitors.
Xuzhou Medical University
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
Second Military Medical University
Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy.
East China University of Science and Technology
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
Xinjiang Technical Institute of Physics and Chemistry
Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety.
Xinxiang Medical University
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
East China University of Science and Technology
Highly Selective and Potentα4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.
Torrey Pines Institute For Molecular Studies
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
Second Military Medical University
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
East China University of Science and Technology
Pyrido[3,2-d]pyrimidine compounds uses thereof for treating a proliferative disease
Université
HETEROARYL AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
Merck Sharp & Dohme
A Crystal Form of a Fluorine-substituted Pyridopyrazole Compound and a Preparation Method Thereof
Jumbo Drug Bank
5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof
Samumed
Oxoalkyl-substituted phenyltriazole derivatives and uses thereof
Bayer Pharma Aktiengesellschaft
Antitumor Activity of Cytotoxic Cyclooxygenase-2 Inhibitors.
Vanderbilt Institute of Chemical Biology, Vanderbilt University School of Medicine
Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie
Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1.
Max Planck Institute of Molecular Physiology
4-phenylpiperazine derivatives with functionalized linkers as dopamine D3 receptor selective ligands and methods of use
The United States of America As Represented By The Secretary of The Department of Health and Human Services
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.
Pfizer
Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.
Case Western Reserve University
OPC-28326, a selective femoral vasodilator, is an alpha2C-adrenoceptor-selective antagonist.
Otsuka Maryland Research Institute
Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.
Universita Di Siena
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.
Abbott Bioresearch Center