80 articles for D Yang
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Discovery of 4-((3'R,4'S,5'R)-6¿-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2¿-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3¿-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Deve
University of Michigan Comprehensive Cancer Center
Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors.
Fudan University
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists.
Shanghai Institute of Materia Medica
Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca(2+)-activated K+ channels.
University College London
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.
University of Michigan
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
University of Michigan
Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization.
Purdue University
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
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
Georgetown University Medical Center
Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.
Purdue University
New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
Cnrs-Biocis
New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor
TBA
Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.
University of Michigan
Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspases.
University of Michigan
Anticancer potential of active alkaloids and synthetic analogs derived from marine invertebrates.
Chengdu University of Traditional Chinese Medicine
Merging Natural Product Structures with Pharmaceutical Leads: Unnatural Enantiomers of Estranes as Glucocorticoid Receptor Modulators That Suppress TNF-α and IL-6 Release.
The Scripps Research Institute
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Merck & Co.
Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader.
Shanghai Institute of Materia Medica
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Astrazeneca
Discovery of novel 7,7-dimethyl-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidines as ATR inhibitors based on structure-based drug design.
Shenyang Pharmaceutical University
Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7.
Shanghaitech University
Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B.
Chengdu Anticancer Bioscience
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University of Michigan
Design and synthesis of HDAC inhibitors to enhance the therapeutic effect of diffuse large B-cell lymphoma by improving metabolic stability and pharmacokinetic characteristics.
China Pharmaceutical University
Design and synthesis of 4-(alpha-hydroxymalonyl)phenylalanine as a new phosphotyrosyl mimetic and its use in growth factor receptor bound 2 src-homology 2 (Grb2 SH2) domain-binding peptides.
National Cancer Institute-Frederick
Recent development of BTK-based dual inhibitors in the treatment of cancers.
Nantong University
Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B.
J. Michael Bishop Institute of Cancer Research
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Astrazeneca
Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands.
National Cancer Institute-Frederick
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.
Arqule
Design, synthesis, and biological evaluation of 2,4-diamino pyrimidine derivatives as potent FAK inhibitors with anti-cancer and anti-angiogenesis activities.
Guizhou Medical University
Utilization of a beta-aminophosphotyrosyl mimetic in the design and synthesis of macrocyclic Grb2 SH2 domain-binding peptides.
National Cancer Institute-Frederick
Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.
National Cancer Institute-Frederick
Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain.
National Cancer Institute-Frederick
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.
National Cancer Institute-Frederick
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.
National Institutes of Health
PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury.
Huazhong University of Science & Technology
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.
University of Michigan
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Lanzhou University
Macrocyclization in the design of a conformationally constrained Grb2 SH2 domain inhibitor.
National Institutes of Health
Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo.
Southern Medical University
Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction as Potential Anticancer Agents.
Southern Medical University
Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes.
Boryung Pharmaceuticals
Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.
National Cancer Institute-Bethesda
Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic.
National Cancer Institute-Bethesda
Recent progress in histone methyltransferase (G9a) inhibitors as anticancer agents.
Southern Medical University
Inhibition of 4-hydroxyphenylpyruvate dioxygenase by sethoxydim, a potent inhibitor of acetyl-coenzyme A carboxylase.
Tunghai Christian University
Tryptophan 2,3-dioxygenase inhibitory activities of tryptanthrin derivatives.
Fudan University
Monocarboxylic-based phosphotyrosyl mimetics in the design of GRB2 SH2 domain inhibitors.
National Cancer Institute-Bethesda
Design, synthesis, biological evaluation, structure-activity relationship, and toxicity of clinafloxacin-azole conjugates as novel antitubercular agents.
Southwest University
Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.
Nankai University
-Benzyl/Aryl Substituted Tryptanthrin as Dual Inhibitors of Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase.
Fudan University
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.
Shenyang Pharmaceutical University
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
Guizhou Medical University
Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
Boryung Pharmaceuticals
Arylcarbamate derivatives of 1-piperidineethanol as potent ligands for 5-HT4 receptors.
Cnrs-Biocis
The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy.
International Institute For Translational Chinese Medicine
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
Boryung Pharmaceuticals
Design, synthesis, and evaluation of novel l-phenylglycine derivatives as potential PPARγ lead compounds.
Southwest University
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities.
Chinese Academy of Sciences
Stabilized β-Hairpin Peptide Inhibits Insulin Degrading Enzyme.
Peking University Shenzhen Graduate School
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.
Shenyang Pharmaceutical University
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity.
Shenyang Pharmaceutical University
Compounds and compositions useful for treating disorders related to NTRK
Blueprint Medicines
JAK kinase inhibitor compounds for treatment of respiratory disease
Theravance Biopharma R&D Ip
Glutathione transferase from Plasmodium falciparum--interaction with malagashanine and selected plant natural products.
University of Zimbabwe
Alicyclic[c] benzopyrone derivatives and uses thereof
Huazhong University of Science & Technology