127 articles for X Hu
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Article Title
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Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors.
Hangzhou Xixi Hospital
Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation.
University of Macau
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
The Hong Kong Polytechnic University
Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold.
University Park Nottingham
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
National Center For Advancing Translational Sciences
Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.
National Center For Advancing Translational Sciences
3-substituted indole inhibitors against Francisella tularensis FabI identified by structure-based virtual screening.
Naval Research Laboratories
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
National Center For Advancing Translational Sciences
Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes.
Research Triangle Institute
Discovery of a novel noniminosugar acida glucosidase chaperone series.
National Center For Advancing Translational Sciences
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor.
Sun Yat-Sen University
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
Pfizer
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.
Pfizer
Novel synthetic inhibitors of selectin-mediated cell adhesion: synthesis of 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-alpha-D- mannopyranosyloxy)phenyl]hexane (TBC1269).
Texas Biotechnology
2-Arylbenzofuran, flavonoid, and tyrosinase inhibitory constituents of Morus yunnanensis.
Fudan University
Separation of Betti Reaction Product Enantiomers: Absolute Configuration and Inhibition of Botulinum Neurotoxin A.
U.S. Army Medical Research Institute For Infectious Diseases
Structural investigation into the inhibitory mechanisms of indomethacin and its analogues towards human glyoxalase I.
Sun Yat-Sen University
Identification of curcumin derivatives as human glyoxalase I inhibitors: A combination of biological evaluation, molecular docking, 3D-QSAR and molecular dynamics simulation studies.
Sun Yat-Sen University
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
Abbott Laboratories
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.
Pfizer
Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations.
Duke University
Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents.
Texas Tech University Health Sciences Center
Natural Product-Inspired Discovery of Naphthoquinone-Furo-Piperidine Derivatives as Novel STAT3 Inhibitors for the Treatment of Triple-Negative Breast Cancer.
Zhejiang University
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
AstraZeneca
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
Targeting kelch-like (KLHL) proteins: achievements, challenges and perspectives.
China Pharmaceutical 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
Casitas b cell lymphoma‑B (Cbl-b): A new therapeutic avenue for small-molecule immunotherapy.
China Pharmaceutical University
Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia.
Zhejiang University
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis.
Zhejiang University
Design and synthesis of the first PARP-1 and proteasome dual inhibitors to treat breast cancer.
Sichuan University
Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies.
Shanghai Institute of Materia Medica
Discovery of a Novel ASM Direct Inhibitor with a 1,5-Diphenyl-pyrazole Scaffold and Its Antidepressant Mechanism of Action.
China Pharmaceutical University
Targeted regulated cell death with small molecule compounds in colorectal cancer: Current perspectives of targeted therapy and molecular mechanisms.
Sichuan University
Discovery of Novel Azaindoles as Potent and Selective PI3Kδ Inhibitors for Treatment of Multiple Sclerosis.
Zhejiang University
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma.
China Pharmaceutical University
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
Abbott Laboratories
Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
Shanghai Institute of Materia Medica
Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer.
Icahn School of Medicine At Mount Sinai
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury.
Zhejiang University
Dual inhibitors of ASK1 and PDK1 kinases: Design, synthesis, molecular docking and mechanism studies of N-benzyl pyridine-2-one containing derivatives as anti-fibrotic agents.
Central South University
Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics.
West China Hospital
Design, synthesis, and biological evaluation of Wee1 kinase degraders.
East China Normal University
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.
Zhejiang University
Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer.
Icahn School of Medicine At Mount Sinai
Recent advances in the design and discovery of synthetic tyrosinase inhibitors.
National Clinical Research Center For Geriatrics
Dammarane-type leads panaxadiol and protopanaxadiol for drug discovery: Biological activity and structural modification.
Shenyang Pharmaceutical University
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
The Johns Hopkins University School of Medicine
The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates.
Peking Union Medical College
-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression.
Lanzhou University
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.
West China Hospital
Evaluation of amentoflavone metabolites on PARP-1 inhibition and the potentiation on anti-proliferative effects of carboplatin in A549 cells.
China Pharmaceutical University
Design, synthesis and biological evaluation of chromone derivatives as novel protein kinase CK2 inhibitors.
China Pharmaceutical University
Optimization of 4-arylthiophene-3-carboxylic acid derivatives as inhibitors of ANO1: Lead optimization studies toward their analgesic efficacy for inflammatory pain.
Peking University
Discovery of novel non-steroidal selective glucocorticoid receptor modulators by structure- and IGN-based virtual screening, structural optimization, and biological evaluation.
Zhejiang University
Discovery of dual inhibitors of topoisomerase I and Cyclooxygenase-2 for colon cancer therapy.
Lanzhou University
Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT.
Zhejiang University
Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size.
The Ohio State University
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.
Sichuan University
N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation.
Lanzhou University
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
Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.
Chinese Academy of Sciences
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer.
Lycera
Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.
Sichuan 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
Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors.
The Ohio State University
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.
Chinese Academy of Sciences
Optimization of ether and aniline based inhibitors of lactate dehydrogenase.
Vanderbilt University
Structure-based design of a macrocyclic inhibitor for peptide deformylase.
The Ohio State University
Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities.
Chongqing Medical University
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.
Hangzhou Institute of Innovative Medicine
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
National Institutes of Health
Lead optimization and efficacy evaluation of quinazoline-based BET family inhibitors for potential treatment of cancer and inflammatory diseases.
National Institutes of Health
Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
Sichuan University and Collaborative Innovation Center
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR
Jiangxi Science & Technology Normal University
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
Zhejiang University
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
Southeast University
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.
Zhejiang University
Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors.
Hong Kong Polytechnic University
Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells.
Jiangxi Science & Technology Normal University
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.
Hangzhou Institute of Innovative Medicine
Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
Wuhan University School of Pharmaceutical Sciences
Spiromastixones A-O, antibacterial chlorodepsidones from a deep-sea-derived Spiromastix sp. fungus.
Peking University
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
Ocean University of China
Dibenzocyclooctadiene lignans: a class of novel inhibitors of multidrug resistance-associated protein 1.
Zhejiang University
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors.
Jiangnan University
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
The University of Texas M.D. Anderson Cancer Center
Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships.
University of Macau
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors.
Jiangnan University
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Karo Pharma
Discovery and lead identification of quinazoline-based BRD4 inhibitors.
National Institutes of Health
Discovery of Novel Flavonoid Dimers To Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "Click Chemistry".
Hong Kong Polytechnic University
Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile.
National Center For Advancing Translational Sciences
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
National Center For Advancing Translational Sciences
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
The University of Texas M.D. Anderson Cancer Center
Discovery of 1,4-Benzodiazepine-2,5-dione (BZD) Derivatives as Dual Nucleotide Binding Oligomerization Domain Containing 1/2 (NOD1/NOD2) Antagonists Sensitizing Paclitaxel (PTX) To Suppress Lewis Lung Carcinoma (LLC) Growth in Vivo.
Peking Union Medical College
CRYSTAL FORM OF 7-AZASPIRO[4,5]DECANE-6,10-DIONE COMPOUND AND PREPARATION METHOD THEREFOR
CMS Research & Development PTE
COMPOUNDS CONTAINING A GEM-DIFLUORIDE GROUP AND PREPARATION METHOD AND USE THEREOF
Cgenetech (Suzhou, China) Co.
SUBSTITUTED N-CYANOPYRROLIDINES WITH ACTIVITY AS USP30 INHIBITORS
Mission Therapeutics
SUBSTITUTED 1-ARYL-1’-HETEROARYL COMPOUNDS, SUBSTITUTED 1,1’-BIHETEROARYL COMPOUNDS, AND METHODS USING SAME
Arbutus Biopharma
COMPOUND AS ADENOSINE A2a RECEPTOR ANTAGONIST AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Chong Kun Dang Pharmaceutical
Methods for treating ulcerative colitis using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile
Theravance Biopharma R&D Ip
1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
Incyte
Synthesis, structure-activity relationships studies of benzoxazinone derivatives as a-chymotrypsin inhibitors.
University of Karachi
Differentiation of 5-hydroxytryptamine2 receptor subtypes using 125I-R-(-)2,5-dimethoxy-4-iodo-phenylisopropylamine and 3H-ketanserin.
Stanford University
Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine a.
University of British Columbia