123 articles for Y Shi
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PMID
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Article Title
Organization
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
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.
Sri International
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.
Bristol-Myers Squibb
Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib.
Xi'An Jiaotong University
Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat.
Arena Pharmaceuticals
Discovery of biphenyl-aryl ureas as novel VEGFR-2 inhibitors. Part 4: exploration of diverse hinge-binding fragments.
Xi'An Jiaotong University
Amino Acid Thioester Derivatives: A Highly Promising Scaffold for the Development of Metallo-ß-lactamase L1 Inhibitors.
North-West University
Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: design, synthesis and 3D-QSAR studies.
Xi'An Jiaotong University
Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Development of oleanane-type triterpenes as a new class of HCV entry inhibitors.
Peking University
Design, synthesis and SAR of piperidyl-oxadiazoles as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Chinese Academy of Sciences
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11ß-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.
TBA
From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.
TBA
Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.
Abbott Laboratories
Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.
Palatin Technologies
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.
Zhejiang University
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Abbott Laboratories
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
Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Abbott Laboratories
Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Abbott Laboratories
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Bristol-Myers Squibb
Synthesis and evaluation of acylguanidine FXa inhibitors.
Bristol-Myers Squibb Research and Development
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Abbott Laboratories
Discovery of novel 5-(2-hydroxyphenyl)-2-phthalide-3(3H)-pyrazolones as balanced multifunctional agents against Alzheimer's disease.
Sichuan University
Novel EGFR inhibitors against resistant L858R/T790M/C797S mutant for intervention of non-small cell lung cancer.
Nankai University
Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies.
University of Chinese Academy of Sciences
Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy.
The Sixth Affiliated Hospital of Wenzhou Medical University
Design and Synthesis of Dual-Targeting Inhibitors of sEH and HDAC6 for the Treatment of Neuropathic Pain and Lipopolysaccharide-Induced Mortality.
Shenyang Pharmaceutical University
Design and synthesis of the first PARP-1 and proteasome dual inhibitors to treat breast cancer.
Sichuan University
Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer.
Shanghai Institute of Materia Medica
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Kymera Therapeutics
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.
Wenzhou Medical University Lishui Hospital
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.
Ningxia Medical University
Application and Study of ROCK Inhibitors in Pulmonary Fibrosis: Recent Developments and Future Perspectives.
Sichuan University
Structure-Directed Discovery of Potent Soluble Epoxide Hydrolase Inhibitors for the Treatment of Inflammatory Diseases.
Shenyang Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Proteolysis-Targeting Chimeras as Highly Selective and Efficient Degraders of Extracellular Signal-Regulated Kinase 5.
Peking University
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.
Shanghai Institute of Materia Medica
Discovery of Novel d-(+)-Biotin-Conjugated Resorcinol Dibenzyl Ether-Based PD-L1 Inhibitors for Targeted Cancer Immunotherapy.
Zunyi Medical University
Evolution and Discovery of Matrine Derivatives as a New Class of Anti-Hepatic Fibrosis Agents Targeting Ewing Sarcoma Breakpoint Region 1 (EWSR1).
Peking Union Medical College
Discovery of Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.
Shenyang Pharmaceutical University
Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.
Ningxia Medical University
Inhibitory effects of phloridzin dihydrate on the activity of mushroom (Agaricus bisporus) tyrosinase.
Xiamen University
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
Chinese Academy of Sciences
Structural Optimization of Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
Shanghai Institute of Materia Medica
Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase-1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation.
China Pharmaceutical University
Matrix metalloproteinases inhibitors in idiopathic pulmonary fibrosis: Medicinal chemistry perspectives.
Sichuan University-University of Oxford Huaxi Joint Centre For Gastrointestinal Cancer
Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist.
Guangzhou Medical University
Annual review of lysine-specific demethylase 1 (LSD1/KDM1A) inhibitors in 2021.
Zhengzhou University
Selective deuteration of bupropion slows epimerization and reduces metabolism.
University of Washington
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism.
Peking Union Medical College
Discovery of novel 3-butyl-6-benzyloxyphthalide Mannich base derivatives as multifunctional agents against Alzheimer's disease.
Sichuan University
Design, synthesis and biological evaluation of 7-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-2,3-dihydro-1H-inden-1-one derivatives as potent FAK inhibitors for the treatment of ovarian cancer.
Sichuan University-University of Oxford Huaxi Joint Centre For Gastrointestinal Cancer
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.
Ningxia Medical University
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease.
Guizhou Medical University
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
University of Science and Technology of China
α/Sulfono-γ-AApeptide Hybrid Analogues of Glucagon with Enhanced Stability and Prolonged In Vivo Activity.
University of South Florida
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1
Bristol Myers Squibb
Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA
Bristol Myers Squibb
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
Identification of Novel Fused Heteroaromatics-Based MALT1 Inhibitors by High-Throughput Screening to Treat B Cell Lymphoma.
Chinese Academy of Sciences
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Janssen Research and Development
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
Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein-Protein Interactions.
University of South Florida
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
Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
Zhejiang University
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Eli Lilly
Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors.
Peking University
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis.
Nankai 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
Glucoconjugated Monoterpene Indole Alkaloids from
Peking University Health Science Center
α-Helix-Mimicking Sulfono-γ-AApeptide Inhibitors for p53-MDM2/MDMX Protein-Protein Interactions.
University of South Florida
Discovery of novel Bcr-Abl inhibitors targeting myristoyl pocket and ATP site.
Xi'An Jiaotong University
Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives.
Xi'An Jiaotong University
Biphenyl derivatives incorporating urea unit as novel VEGFR-2 inhibitors: design, synthesis and biological evaluation.
Xi'An Jiaotong University
Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers.
Zhejiang University
Synthesis and antityrosinase activities of alkyl 3,4-dihydroxybenzoates.
Xiamen University
Structure-based optimization of click-based histone deacetylase inhibitors.
Nankai University
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Qbi Covid-19 Research Group (Qcrg)
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.
Peking University
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.
Wuxi Apptec (Shanghai)
Brain penetrant kinase inhibitors: Learning from kinase neuroscience discovery.
Eli Lilly
Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis.
East China Normal University
Structure, synthesis and biological properties of the pentacyclic guanidinium alkaloids.
Nc State University
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.
Nankai University
One-Bead-Two-Compound Thioether Bridged Macrocyclicγ-AApeptide Screening Library against EphA2.
University of South Florida
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma
Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6h)-ones
Dart Neuroscience (Cayman)
Tripeptides with non-code amino acids as potential serine proteases inhibitors.
Medical University of Bialystok
Potent and Selective EphA4 Agonists for the Treatment of ALS.
Sanford Burnham Prebys Medical Discovery Institute
Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
Boehringer Ingelheim International
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.
University of Toronto
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.
UniversitÉ
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.
Vertex Pharmaceuticals
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
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
National Institutes of Health
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles.
Wyeth Research
The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.
Merck Research Laboratories
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Merck Research Laboratories