84 articles for H Zhu
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PMID
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Article Title
Organization
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Abbvie
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Novartis Institutes For Biomedical Research
Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.
Abbvie
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
Intra-Cellular Therapies
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
University of Illinois At Chicago
In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.
Fudan University
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo
Pfizer
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Intra-Cellular Therapies
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Pfizer
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Genentech
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
East China Normal University
Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.
Abbott Laboratories
Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.
Genentech
Synthesis, molecular modeling and biological evaluation of 2-aminomethyl-5-(quinolin-2-yl)-1,3,4-oxadiazole-2(3H)-thione quinolone derivatives as novel anticancer agent.
Shandong University of Technology
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Genentech
A novel aminopeptidase N inhibitor developed by virtual screening approach.
Shandong Academy of Sciences
Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.
Genentech
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).
Shandong University
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration.
Targegen
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
Targegen
Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.
Pfizer
Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione.
Shandong University
Novel matrix metalloproteinase inhibitors derived from quinoxalinone scaffold (Part I).
Shandong University
Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13.
Shandong University
A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.
Merck Research Laboratories
Design, synthesis and primary activity evaluation of L-arginine derivatives as amino-peptidase N/CD13 inhibitors.
Shandong University
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Merck Research Laboratories
Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors.
Shandong University
Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold.
Shandong University
Design, synthesis, and QSAR studies of novel lysine derives as amino-peptidase N/CD13 inhibitors.
Shandong University
Synthesis and bioevaluation of novel stilbene-based derivatives as tubulin/HDAC dual-target inhibitors with potent antitumor activities in vitro and in vivo.
China Pharmaceutical University
Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension.
China Pharmaceutical University
Discovery of N'-benzyl-3-chloro-N-((1S,3R,4R)-3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)cyclohexyl)benzenesulfonamide as a novel selective KOR ligand.
Fudan University
Synthesis and evaluation of neuroactive steroids with novel pharmacophore at C-21 let identify a compound with advantageous PK profile and higher EC50 and Emax as PAM on GABAA receptor.
Yantai University
Undobolins A-L, Ophiobolin-Type Sesterterpenoids from Aspergillus undulatus.
Huazhong University of Science and Technology
Accelerated Discovery of Carbamate Cbl-b Inhibitors Using Generative AI Models and Structure-Based Drug Design.
AstraZeneca
Recent progress and applications of small molecule inhibitors of Keap1-Nrf2 axis for neurodegenerative diseases.
Hangzhou City University
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.
Targegen
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Discovery of Oral AMP-Activated Protein Kinase Activators for Treating Hyperlipidemia.
Chinese Academy of Medical Sciences and Peking Union Medical College
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.
Merck
Discovery of novel hypoxia-activated, nitroimidazole constructed multi-target kinase inhibitors on the basis of AZD9291 for the treatment of human lung cancer.
Hangzhou City University
Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors.
Xinxiang Medical University
The lipidation and glycosylation enabling bioactivity enhancement and structural change of antibacterial peptide G3.
Fujian Normal University
Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.
Zhejiang University
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.
Zhejiang University
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
China Pharmaceutical University
Glycosylation increases the anti-QS as well as anti-biofilm and anti-adhesion ability of the cyclo (L-Trp-L-Ser) against Pseudomonas aeruginosa.
Fujian Normal University
Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of quinazoline derivatives as potent and selective FGFR4 inhibitors.
Zhejiang University
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
Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.
Chinese Academy of Sciences
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
University of Illinois At Chicago
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
National Institutes of Health
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Novartis Institutes For Biomedical Research
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.
Hangzhou Xixi Hospital
Flavipesines A and B and Asperchalasines E-H: Cytochalasans and Merocytochalasans from
Huazhong University of Science and Technology
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.
Lanzhou University
Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.
Genentech
Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
Wuyi University
Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src.
Purdue University
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Pfizer
BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.
Huazhong University of Science and Technology
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Merck
Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.
Nankai University
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.
Shanghai Jiao Tong University
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
Nanjing University of Chinese Medicine
Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2.
Guizhou Medical University
Tricyclic Polyprenylated Acylphloroglucinols from St John's Wort, Hypericum perforatum.
Chinese Academy of Sciences
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Merck
Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
National Center For Advancing Translational Sciences
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin
Wuxi Apptec
Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors
Merck Sharp & Dohme