172 articles for H Jiang
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Article Title
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Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.
Shandong University
Discovery of novel BRD4 inhibitors by high-throughput screening, crystallography, and cell-based assays.
Nanchang University
Novel ferulic amide derivatives with tertiary amine side chain as acetylcholinesterase and butyrylcholinesterase inhibitors: The influence of carbon spacer length, alkylamine and aromatic group.
Hu'Nan 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
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea
Chinese Academy of Sciences
Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening.
Shanghai University
Discovery, synthesis and biological evaluation of 2-(4-(N-phenethylsulfamoyl)phenoxy)acetamides (SAPAs) as novel sphingomyelin synthase 1 inhibitors.
Fudan University
Inhibition of Cancer-Associated Mutant Isocitrate Dehydrogenases by 2-Thiohydantoin Compounds.
Baylor College of Medicine
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
Shanghai Institute of Materia Medica
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.
Chinese Academy of Sciences
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
Second Military Medical University
Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.
China Pharmaceutical University
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
Chinese Academy of Sciences
Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening.
Chinese Academy of Sciences
Discovery of two aminoglycoside antibiotics as inhibitors targeting the menin-mixed lineage leukaemia interface.
Fuzhou University
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.
Chinese Academy of Sciences
Thermodynamic and structural characterization of halogen bonding in protein-ligand interactions: a case study of PDE5 and its inhibitors.
Chinese Academy of Sciences (Cas)
Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.
Chinese Academy of Sciences
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.
Chinese Academy of Sciences
Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase.
Baylor College of Medicine
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.
Chinese Academy of Sciences
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
Chinese Academy of Sciences
Discovery and mechanism study of SIRT1 activators that promote the deacetylation of fluorophore-labeled substrate.
Chinese Academy of Sciences
Anthraquinone Derivatives as Potent Inhibitors of c-Met Kinase and the Extracellular Signaling Pathway.
Soochow University
Identification of benzofuran-3-yl(phenyl)methanones as novel SIRT1 inhibitors: binding mode, inhibitory mechanism and biological action.
Chinese Academy of Sciences
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
Chinese Academy of Sciences
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Chinese Academy of Sciences
Multitarget-directed benzylideneindanone derivatives: anti-ß-amyloid (Aß) aggregation, antioxidant, metal chelation, and monoamine oxidase B (MAO-B) inhibition properties against Alzheimer's disease.
Sun Yat-Sen University
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Georgia State University
Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.
Baylor College of Medicine
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.
Chinese Academy of Sciences
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor.
Shenyang Pharmaceutical University
Natural products as a gold mine for selective matrix metalloproteinases inhibitors.
East China University of Science and Technology
A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions.
Southern Medical University
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.
Chinese Academy of Sciences
Photoregulation of thrombin aptamer activity using Bhc caging strategy.
University of Science and Technology of China
Novel thiophene derivatives as PTP1B inhibitors with selectivity and cellular activity.
Chinese Academy of Sciences
Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Graduate School of The Chinese Academy of Sciences
Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation.
Graduate School of The Chinese Academy of Sciences
Simultaneous identification of multiple receptors of natural product using an optimized cDNA phage display cloning.
Chinese Academy of Sciences
Discovery of Helicobacter pylori shikimate kinase inhibitors: bioassay and molecular modeling.
Chinese Academy of Sciences
Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).
Fudan University
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).
Fudan University
Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
Eli Lilly
Synthesis and acetylcholinesterase inhibitory activity of (+/-)-14-fluorohuperzine A.
Chinese Academy of Sciences
Discovery of novel selective inhibitors for EGFR-T790M/L858R.
Dalian University of Technology
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
Guangzhou Institute of Biomedicine and Health
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
TBA
Design and synthesis of small molecule RhoA inhibitors: a new promising therapy for cardiovascular diseases?
East China University of Science and Technology
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.
Chinese Academy of Sciences
Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay.
Singapore Polytechnic
Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase.
Chinese Academy of Sciences
SHAFTS: a hybrid approach for 3D molecular similarity calculation. 2. Prospective case study in the discovery of diverse p90 ribosomal S6 protein kinase 2 inhibitors to suppress cell migration.
East China University of Science and Technology
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Chinese Academy of Sciences
A series of alpha-heterocyclic carboxaldehyde thiosemicarbazones inhibit topoisomerase IIalpha catalytic activity.
Chinese Academy of Sciences
Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.
Chinese Academy of Sciences
Discovering potent small molecule inhibitors of cyclophilin A using de novo drug design approach.
East China University of Science and Technology
Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors.
Chinese Academy of Sciences
Halogen bonding--a novel interaction for rational drug design?
Chinese Academy of Sciences
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
Metabasis Therapeutics
Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.
Institute of Materia Medica
Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.
Metabasis Therapeutics
AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo.
Shanghai Institute of Materia Medica
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists.
Nanjing University of Chinese Medicine
Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response.
Xuzhou Medical University
Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
Skyrun Pharma Co.
Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.
Chinese Academy of Sciences
Pleiotropic effects of a mitochondrion-targeted glutathione reductase inhibitor on restraining tumor cells.
The Affiliated Hospital of Qingdao University
Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC.
Nanchang University
Design, Synthesis, and Biological Evaluation of Bipyridazine Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
Fudan University
Synthesis and biological evaluation of novel pteridin-7(8H)-one derivatives as potent CDK2 inhibitors.
Jiangnan University
Design, synthesis and biological evaluation of quinazoline SOS1 inhibitors.
Jiangnan University
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
Chinese Academy of Sciences
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
Peking Union Medical College
Discovery of 4-((E)-3,5-dimethoxy-2-((E)-2-nitrovinyl)styryl)aniline derivatives as potent and orally active NLRP3 inflammasome inhibitors for colitis.
School of Pharmacy Anhui Medical University
Species-Selective Targeting of Fungal Hsp90: Design, Synthesis, and Evaluation of Novel 4,5-Diarylisoxazole Derivatives for the Combination Treatment of Azole-Resistant Candidiasis.
Shenyang Pharmaceutical University
Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
Shenyang Pharmaceutical University
Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.
Shanghai Institute of Materia Medica
Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation.
Jiangnan University
Niemann-Pick C1-Like 1 inhibitors for reducing cholesterol absorption.
The Affiliated Hospital of Qingdao University
Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.
Peking Union Medical College
Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction.
Nanjing University of Chinese Medicine
Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites.
Huazhong Agricultural University
Identification and In Silico Binding Study of a Highly Potent DENV NS2B-NS3 Covalent Inhibitor.
Shenyang Pharmaceutical University
Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1).
Chinese Academy of Sciences
LXR-Mediated Regulation of Marine-Derived Piericidins Aggravates High-Cholesterol Diet-Induced Cholesterol Metabolism Disorder in Mice.
Southern Medical University
Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy.
Peking Union Medical College
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A
Shanghaitech University
Design, synthesis, and structure-activity relationships of haloenol lactones: site-directed and isozyme-selective glutathione S-transferase inhibitors.
Chinese Academy of Sciences
Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity.
Zhejiang Ocean University
Dynamics of Post-Translational Modification Inspires Drug Design in the Kinase Family.
Soochow University
Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
Shenyang Pharmaceutical University
Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.
Fujian Medical University
Discovery of novel reversible monoacylglycerol lipase inhibitors via docking-based virtual screening.
Nanchang University
Discovery and characterization of a novel glucose-6-phosphate dehydrogenase (G6PD) inhibitor via high-throughput screening.
Nanjing University of Chinese Medicine
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
Chinese Academy of Sciences
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I
Gilead Sciences
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.
Shanghaitech University
Molecular docking and 3D-QSAR studies on gag peptide analogue inhibitors interacting with human cyclophilin A.
Chinese Academy of Sciences
Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.
Washington University School of Medicine
Automated design and optimization of multitarget schizophrenia drug candidates by deep learning.
Shanghai Institute of Materia Medica
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.
Chinese Academy of Sciences
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models.
Chinese Academy of Sciences
Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors.
Xiamen University
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes.
East China University of Science and Technology
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation.
Shanghai Institute of Materia Medica
Synthesis and acetylcholinesterase inhibitory activity of huperzine A-E2020 combined compound.
Institute of Materia Medica
Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer.
Chinese Academy of Sciences
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
Ophiobolin-Type Sesterterpenoids from the Mangrove Endophytic Fungus
Sun Yat-Sen University
Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors.
Shanghai Institute of Materia Medica
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.
University of Chinese Academy of Sciences
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Chinese Academy of Sciences
Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.
Chinese Academy of Sciences
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors.
Chinese Academy of Sciences
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
China Pharmaceutical University
Discovery of Novel Disruptor of Silencing Telomeric 1-Like (DOT1L) Inhibitors using a Target-Specific Scoring Function for the (S)-Adenosyl-l-methionine (SAM)-Dependent Methyltransferase Family.
Chinese Academy of Sciences
Identification, synthesis and pharmacological evaluation of novel anti-EV71 agents via cyclophilin A inhibition.
East China University of Science and Technology
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.
Chinese Academy of Sciences
Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.
Central South University
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
Chinese Academy of Sciences
Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
Chinese Academy of Sciences
Discovering potassium channel blockers from synthetic compound database by using structure-based virtual screening in conjunction with electrophysiological assay.
Chinese Academy of Sciences
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.
Chinese Academy of Sciences
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.
Shanghai Institute of Materia Medica
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.
University of Chinese Academy of Sciences
Discovery of potent DOT1L inhibitors by AlphaLISA based High Throughput Screening assay.
University of Science and Technology of China
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.
University of Chinese Academy of Sciences
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
East China University of Science and Technology
Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.
Hebei University
Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening.
Shanghai University
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Design, synthesis and biological evaluation of 4,7,12,12a-tetrahydro-5H-thieno[3',2':3,4]pyrido[1,2-b]isoquinolines as novel adenosine 5'-monophosphate-activated protein kinase (AMPK) indirect activators for the treatment of type 2 diabetes.
Shanghai Institute of Materia Medica
Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.
West China Hospital of Sichuan University
Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation.
Zhejiang Sci-Tech University
Pyrido[3,2-d]pyrimidine compounds uses thereof for treating a proliferative disease
Université
INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS LIPOAMIDE DEHYDROGENASE
Cornell University
Pyrido[2,3-D]Imidazole Derivatives and Their Use As Inhibitors of ITK for the Treatment of Skin Disease
Pfizer
5-[3-[piperazin-1-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS 4 and 5 inhibitors for treating e.g. osteoarthritis
Galapagos
Combination of respiratory electron transport chain inhibitors with a cytochrome bd inhibitor
TBA
Methods and compositions for cell-proliferation-related disorders
Agios Pharmaceuticals
Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Pfizer
Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli.
Astrazeneca India
Characterisation of the melanocortin 4 receptor by radioligand binding.
Uppsala University
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Merck Research Laboratories
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Sphinx Laboratories