148 articles for R Zhang
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Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Merck
Discovery of novel DNA methyltransferase 3A inhibitors via structure-based virtual screening and biological assays.
University of Science and Technology of China
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.
Bristol-Myers Squibb
Synthesis and evaluation of novel angiotensin II receptor 1 antagonists as anti-hypertension drugs.
Donghua University
Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Beijing Pearl Biotech
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Beijing Pearl Biotech
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
Merck Research Laboratories
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
Chinese Academy of Sciences
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Merck Research Laboratories
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.
Merck Research Laboratories
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.
Janssen Research and Development
Anthraquinone Derivatives as Potent Inhibitors of c-Met Kinase and the Extracellular Signaling Pathway.
Soochow University
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Chinese Academy of Sciences
Synthesis and bioactivity of substituted indan-1-ylideneaminoguanidine derivatives.
China Pharmaceutical University
Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway.
Novartis Institutes For Biomedical Research
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Bristol-Myers Squibb
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Bristol-Myers Squibb Research and Development
Activation of inhibitors by sortase triggers irreversible modification of the active site.
University of Chicago
Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones.
Novartis Institutes For Biomedical Research
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Bristol-Myers Squibb Pharmaceutical Research Institute
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Bristol-Myers Squibb Pharmaceutical Research Institute
Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.
Bristol-Myers Squibb
5-amino-pyrazoles as potent and selective p38a inhibitors.
Bristol-Myers Squibb Research and Development
Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38a MAP kinase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.
Bristol-Myers Squibb R & D
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
Bristol-Myers Squibb
The structure-based design, synthesis, and biological evaluation of DNA-binding amide linked bisintercalating bisanthrapyrazole anticancer compounds.
University of Manitoba
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Novartis Institutes For Biomedical Research
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.
National Center For Drug Screening
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Bristol-Myers Squibb
Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents.
Texas Tech University Health Sciences Center
Assessment of the structure-activity relationship and antileukemic activity of diacylpyramide compounds as human ClpP agonists.
University of Chinese Academy of Sciences
Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase.
Soochow University
Discovery of DNL343: A Potent, Selective, and Brain-Penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases.
Denali Therapeutics Inc.
Discovery, Optimization, and Evaluation of Novel Pyridin-2(1H)-one Analogues as Potent TRK Inhibitors for Cancer Treatment.
Shanghai Tech University
Design and Synthesis of Dual-Target Inhibitors Targeting Androgen Receptors and Glucocorticoid Receptors to Overcome Antiandrogen Resistance in Castration-Resistant Prostate Cancer.
Zhejiang Normal University
Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease.
Shenyang Pharmaceutical University
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Merck & Co.
Strategies of targeting CYP51 for IFIs therapy: Emerging prospects, opportunities and challenges.
Sichuan University
Targeting SARS-CoV-2 entry processes: The promising potential and future of host-targeted small-molecule inhibitors.
National Clinical Research Center for Geriatrics
Recent Progress and Prospects of Small Molecules for NLRP3 Inflammasome Inhibition.
Sichuan University
Synthesis and Bioevaluation of 3-(Arylmethylene)indole Derivatives: Discovery of a Novel ALK Modulator with Antiglioblastoma Activities.
Nanjing Medical University
Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.
Johnson and Johnson Pharmaceutical Research and Development
Discovery of pyrimidine-5-carboxamide derivatives as novel salt-inducible kinases (SIKs) inhibitors for inflammatory bowel disease (IBD) treatment.
Sichuan University
Discovery of Triazinone Derivatives as Novel, Specific, and Direct NLRP3 Inflammasome Inhibitors for the Treatment of DSS-Induced Ulcerative Colitis.
Sichuan University
Design, Synthesis, and Biological Evaluation of Novel P2X7 Receptor Antagonists for the Treatment of Septic Acute Kidney Injury.
Sichuan University
From lead to clinic: A review of the structural design of P2X7R antagonists.
Sichuan University
Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP).
Nanjing University of Chinese Medicine
Discovery, synthesis and mechanism study of 2,3,5-substituted [1,2,4]-thiadiazoles as covalent inhibitors targeting 3C-Like protease of SARS-CoV-2.
Shanghaitech University
Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist.
Yantai University
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.
China Pharmaceutical University
Identification of a Selective SCoR2 Inhibitor That Protects Against Acute Kidney Injury.
Case Western Reserve University School of Medicine
Synthesis and anticancer activity of novel histone deacetylase inhibitors that inhibit autophagy and induce apoptosis.
Wuyi University
Pleiotropic effects of a mitochondrion-targeted glutathione reductase inhibitor on restraining tumor cells.
The Affiliated Hospital of Qingdao University
Discovery of Thieno[3,2-d]pyrimidine derivatives as potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) kinase.
China Pharmaceutical University
Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents.
Northwest A&F University
An ATG4B inhibitor blocks autophagy and sensitizes Sorafenib inhibition activities in HCC tumor cells.
Yantai University
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Merck Research Laboratories
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Merck
Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis.
Denali Therapeutics
Identification of the gossypol derivatives as androgen receptor inhibitor.
Zhejiang Normal University
Optimization of NAMPT activators to achieve in vivo neuroprotective efficacy.
School of Pharmaceutical Sciences
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring.
Abbott Laboratories
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides.
Abbott Laboratories
Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.
Eternity Bioscience
Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
Yantai University
Niemann-Pick C1-Like 1 inhibitors for reducing cholesterol absorption.
The Affiliated Hospital of Qingdao University
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.
Abbott Laboratories
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Bristol-Myers Squibb
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 2-(Ortho-Substituted Benzyl)-Indole Derivatives as Potent and Orally Bioavailable RORγ Agonists with Antitumor Activity.
Shanghai Hengrui Pharmaceutical
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
TBA
Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers.
Eternity Bioscience
Dual-Targeting Antiproliferation Hybrids Derived from 1-Deoxynojirimycin and Kaempferol Induce MCF-7 Cell Apoptosis through the Mitochondria-Mediated Pathway.
Jiangsu University of Science and Technology
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.
Lanzhou University
Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors.
Shenyang Pharmaceutical University
Design, synthesis and biological activities of benzo[d]imidazo[1,2-a]imidazole derivatives as TRPM2-specfic inhibitors.
Peking University
Discovery of a new class of JMJD6 inhibitors and structure-activity relationship study.
Nankai University
Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
Anhui Medical University
Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D.
Nankai University
Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.
Zhejiang University
Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
Yantai University
Application of the lambda-dynamics method to evaluate the relative binding free energies of inhibitors to HCV protease.
Schering-Plough Research Institute
Design, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment.
Chinese Academy of Sciences
One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
The Affiliated Hospital of Qingdao University
Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer.
Texas Tech University Health Sciences Center
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities.
Lanzhou University
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.
Lanzhou University
Azapeptides as inhibitors of the hepatitis C virus NS3 serine protease.
Schering-Plough Research Institute
Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.
Bristol-Myers Squibb Pharmaceutical Research Institute
Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist.
Zhejiang Normal University
Lead discovery, chemical optimization, and biological evaluation studies of novel histone methyltransferase SET7 small-molecule inhibitors.
University of Chinese Academy of Sciences
Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.
Shandong Provincial Hospital Affiliated To Shandong University
Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.
Merck Research Laboratories
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
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Chinese Academy of Sciences
Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.
Janssen Research & Development
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR
Jinan University
The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening.
Zhejiang Sci-Tech University
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.
Lanzhou University
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Chinese Academy of Sciences
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors.
Chinese Academy of Sciences
The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Bristol-Myers Squibb Pharmaceutical Research Institute
CoMFA and CoMSIA 3D-QSAR studies on quionolone caroxylic acid derivatives inhibitors of HIV-1 integrase.
Lanzhou University
QSAR models for 2-amino-6-arylsulfonylbenzonitriles and congeners HIV-1 reverse transcriptase inhibitors based on linear and nonlinear regression methods.
Lanzhou University
Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening.
Chinese Academy of Sciences
Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors.
Chinese Academy of Sciences
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Bristol-Myers Squibb
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.
Merck
PYRAZOLE MEMBRANE-ASSOCIATED TYROSINE-AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
Insilico Medicine Ip
FUSED BICYCLIC SUBSTITUTED N-(1H-INDOL-7-YL)BENZENESULFONAMIDES AND USES THEREOF
Triana Biomedicines
Pyridine quinoline compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
Shionogi
Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
Array Biopharma
Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie
Synthesis of novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene derivatives and their biological evaluation against protein tyrosine phosphatase 1B.
Jiangnan University
Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs.
TBA
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.
Alcon Research
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.
Eli Lilly