112 articles for R Wang
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Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines.
Georgia State University
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.
East China University of Science and Technology
Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new ROR¿ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation.
Jilin University
Discovery of novel N,N-3-phenyl-3-benzylaminopropionanilides as potent inhibitors of cholesteryl ester transfer protein in vivo.
Shenyang Pharmaceutical University
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
Lanzhou University
Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Merck Research Laboratories
Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO).
Zhengzhou University
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.
Amri
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase.
East China University of Science and Techology
Design, synthesis and docking study of novel tetracyclic oxindole derivatives asa-glucosidase inhibitors.
Key Laboratory of Industrial Fermentation Microbiology (Tianjin University of Science and Technology)
Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors.
Shenyang Pharmaceutical University
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
Chinese Academy of Sciences
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.
Pfizer
Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1.
Chinese Academy of Sciences
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives.
Key Laboratory of Medicinal Chemistry For Natural Resource (Yunnan University)
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Pfizer
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.
Glaxosmithkline
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).
Lanzhou University
Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group.
TBA
X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.
Sanofi Us
Human kallikrein 6 inhibitors with a para-amidobenzylanmine P1 group identified through virtual screening.
Sanofi Pharmaceuticals
Novel oxadiazole analogues derived from ethacrynic acid: design, synthesis, and structure-activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation.
Shandong University
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Abbott Laboratories
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
University of Michigan Comprehensive Cancer Center
Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.
Wayne State University School of Medicine
Effects ofß-glucosidase hydrolyzed products of harpagide and harpagoside on cyclooxygenase-2 (COX-2) in vitro.
Shanghai University of Traditional Chinese Medicine
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Merck Research Laboratories
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
Pfizer
Synthesis and anti-tumor activities of methyl 2-O-aryl-6-O-aryl'-D-glucopyranosides.
Ocean University of China
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.
Lanzhou University
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors.
Glaxosmithkline
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Merck Research Laboratories
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring.
Chinese Academy of Sciences
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Lanzhou University
Discovery of novel dihydropyrrolidone-thiadiazole compound crosstalk between the YycG/F two-component regulatory pathway and cell membrane homeostasis to combat methicillin-resistant Staphylococcus aureus.
Nanjing Tech University
Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease.
Northwest A&F University
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs.
George Washington University
Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy.
Tongji University
Target identification, and optimization of dioxygenated amide derivatives as potent antibacterial agents with FabH inhibitory activity.
Anhui University of Chinese Medicine
Design and synthesis of dual BRD4/Src inhibitors for treatment of triple-negative breast cancer.
Shenzhen University
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.
Wenzhou Medical University
Pyrrole-containing hybrids as potential anticancer agents: An insight into current developments and structure-activity relationships.
Jiangxi Science & Technology Normal University
Development of novel hydrazidoarylaminopyrimidine-based BTK/FLT3 dual inhibitors with potent in vivo anti-hematological malignancies effects.
Nantong University
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
University of Michigan
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
University of Michigan
Discovery and Design of Novel Cyclic Peptides as Specific Inhibitors Targeting CCN2 and Disrupting CCN2/EGFR Interaction for Kidney Fibrosis Treatment.
Sun Yat-Sen University
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
Abbott Laboratories
Design, synthesis, and biological evaluation of diaminopyrimidine derivatives as novel focal adhesion kinase inhibitors.
Shenyang Pharmaceutical University
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.
Abbott Laboratories
Discovery, Optimization, and Evaluation of Novel
Chinese Academy of Medical Sciences & Peking Union Medical College
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.
Abbott Laboratories
Discovery of Highly Selective Inhibitors of the Human Constitutive Proteasome β5c Chymotryptic Subunit.
Weill Cornell Medicine
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Lanzhou University
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Nankai University
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Gilead Sciences
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University of Michigan
Synthesis and Biological Evaluation of Celastrol Derivatives with Improved Cytotoxic Selectivity and Antitumor Activities.
China Pharmaceutical University
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Abbott Laboratories
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.
Lanzhou University
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
Chinese Academy of Sciences
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.
Shenyang Pharmaceutical University
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.
Merck
Evaluation of amentoflavone metabolites on PARP-1 inhibition and the potentiation on anti-proliferative effects of carboplatin in A549 cells.
China Pharmaceutical University
Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study.
Shenyang Pharmaceutical University
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Lanzhou University
Optimization of Beclin 1-Targeting Stapled Peptides by Staple Scanning Leads to Enhanced Antiproliferative Potency in Cancer Cells.
Fudan University
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Glaxosmithkline
Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer.
China Pharmaceutical University
Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors.
Shenyang Pharmaceutical University
Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
Lanzhou University
Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.
Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
Jiangxi University of Traditional Chinese Medicine
Discovery of novel VEGFR-2 inhibitors embedding 6,7-dimethoxyquinazoline and diarylamide fragments.
China Pharmaceutical University
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.
Merck Research Laboratories
Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities.
Lanzhou University
Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.
Weill Cornell Medicine
Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.
Shenyang Pharmaceutical University
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Lanzhou University
A cell-based fluorescent assay for FAP inhibitor discovery.
Peking University First Hospital
Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase.
Tongji University
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes.
East China University of Science and Technology
2-(4-Fluorophenyl)-quinazolin-4(3H)-one as a novel tyrosinase inhibitor: Synthesis, inhibitory activity, and mechanism.
Jiangxi Normal University
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agent Targeting Transforming Growth Factor β Type I Receptor.
Sun Yat-Sen 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 an EGFR tyrosine kinase inhibitor from Ilex latifolia in breast cancer therapy.
Wannan Medical College
Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents.
Shenyang Pharmaceutical University
Recent advances on synthesis and biological activities of aurones.
Northwest A&F University
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
Peking University
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Peking University
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
Mcgill University
Novel Highly Potent and Metabolically Resistant Oxoeicosanoid (OXE) Receptor Antagonists That Block the Actions of the Granulocyte Chemoattractant 5-Oxo-6,8,11,14-Eicosatetraenoic Acid (5-oxo-ETE).
Florida Institute of Technology
Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.
Guangzhou Medical University
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Abbvie
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.
Chinese Academy of Sciences
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Abbvie
Structure-activity relationship study ofβ-oxidation resistant indole-based 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE) receptor antagonists.
Florida Institute of Technology
Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.
Shenyang Pharmaceutical University
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Abbvie
Benzene disulfonamide for the treatment of cancer
Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften
Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.
Shandong University