131 articles for L Huang
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Amgen
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
Sun Yat-Sen University
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.
Peking Union Medical College
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
Huazhong University of Science and Technology
Synthesis and evaluation of selegiline derivatives as monoamine oxidase inhibitor, antioxidant and metal chelator against Alzheimer's disease.
Sun Yat-Sen University
Discovery of novel non-covalent inhibitors selective to theß5-subunit of the human 20S proteasome.
Peking Union Medical College
Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.
University of Pennsylvania
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
University of Pennsylvania
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
China Pharmaceutical University
Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease.
Sun Yat-Sen University
Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
Design, synthesis and evaluation of dual pharmacologyß2-adrenoceptor agonists and PDE4 inhibitors.
Sun Yat-Sen University
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Amgen
Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity.
Sun Yat-Sen University
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
Sun Yat-Sen University
Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen.
Sun Yat-Sen University
Synthesis and biological evaluation of berberine-thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and Aß aggregation and antioxidant activity.
Sun Yat-Sen University
Design, synthesis, and evaluation of multitarget-directed resveratrol derivatives for the treatment of Alzheimer's disease.
Sun Yat-Sen University
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.
Sun Yat-Sen University
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dualß2-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.
Sun Yat-Sen University
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
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
O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-ß aggregation.
Sun Yat-Sen University
Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.
Sun Yat-Sen University
Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes.
Sichuan University
Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids.
Sun Yat-Sen University
The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.
Amgen
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
Amgen
Design, synthesis, and biological evaluation of semicarbazide-sensitive amine oxidase (SSAO) inhibitors with anti-inflammatory activity.
La Jolla Pharmaceutical
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.
University of North Carolina
Dualß2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
Sun Yat-Sen University
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Amgen
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
Guangzhou Institute of Biomedicine and Health
Synthesis, biological evaluation of 9-N-substituted berberine derivatives as multi-functional agents of antioxidant, inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-ß aggregation.
Sun Yat-Sen University
Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.
University of Pennsylvania
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Discovery and SAR of methylated tetrahydropyranyl derivatives as inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT).
Myrexis
Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4.
University of Pennsylvania
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors.
Sun Yat-Sen University
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.
Sun Yat-Sen University
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
Sun Yat-Sen University
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.
Shanghai Hengrui Pharmaceuticals
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
Sun Yat-Sen University
Zaragozic Acids D and D2: Potent Inhibitors of Squalene Synthase and of Ras Farnesyl-Protein Transferase
TBA
Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
Amgen
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Amgen
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.
Xiamen University
Design, synthesis and biological evaluation of novel DCLK1 inhibitor containing purine skeleton for the treatment of pancreatic cancer.
China Pharmaceutical University
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.
Ocean University of China
Discovery of Imidazo[1,2-a]pyrazine Derivatives as Potent ENPP1 Inhibitors.
Shanghai Institute of Materia Medica
Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment.
China Pharmaceutical University
Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in vivo.
Sichuan University
Identifying Marine-Derived Tanzawaic Acid Derivatives as Novel Inhibitors against Osteoclastogenesis and Osteoporosis via Downregulation of NF-κB and NFATc1 Activation.
Chinese Academy of Sciences
Dual Antagonism of α9α10 nAChR and GABAB Receptor-Coupled CaV2.2 Channels by an Analgesic αO-Conotoxin Analogue.
Ocean University of China
Design, Synthesis, and Evaluation of the Selective and Orally Active LSD1 Inhibitor with the Potential of Treating Heart Failure.
Zhengzhou University
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
China Pharmaceutical University
Heterocyclic-Modified Imidazoquinoline Derivatives: Selective TLR7 Agonist Regulates Tumor Microenvironment against Melanoma.
Southern Medical University
Novel small molecule inhibitors targeting renal cell carcinoma: Status, challenges, future directions.
Sichuan University
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors.
Sichuan University
Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong
University of Michigan
Discovery of the Potent and Highly Selective PARP7 Inhibitor as a Novel Immunotherapeutic Agent for Tumors.
China Pharmaceutical University
The importance of indole and azaindole scaffold in the development of antitumor agents.
Qingdao University of Science and Technology
Discovery of the First Selective IDO2 Inhibitor As Novel Immunotherapeutic Avenues for Rheumatoid Arthritis.
China Pharmaceutical University
Identification of N, C-capped di- and tripeptides as selective immunoproteasome inhibitors.
Peking Union Medical College
Novel non-benzimidazole chk2 kinase inhibitors.
Johnson and Johnson Pharmaceutical Research and Development
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.
Nanjing University
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
Shanghai Institute of Technology
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
Peking Union Medical College
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.
China Pharmaceutical University
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.
University of Michigan
Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype.
Bristol Myers Squibb Research and Development
Discovery and Evaluation of Pyrazolo[3,4-
Hubei Bio-Pharmaceutical Industrial Technological Institute
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
Jiangsu Ocean University
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.
University of California
Discovery and structure-activity relationship studies of 1-aryl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione derivatives as potent dual inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1) and trytophan 2,3-dioxygenase (TDO).
Sichuan University
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
University of California
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Merck
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Haisco Pharmaceutical Group
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6
Harvard Medical School
Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
Sun Yat-Sen University
Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Guangzhou University of Chinese Medicine
A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45.
Ningbo University
Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids.
Sun Yat-Sen University
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.
TBA
The discovery of a potent and selective third-generation EGFR kinase inhibitor as a therapy for EGFR L858R/T790M double mutant non-small cell lung cancer.
Sun Yat-Sen University
Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.
Toho University
Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.
TBA
TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.
East China Normal University
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Sichuan University
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong
TBA
Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABA
Qingdao University of Science and Technology
Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
Beijing Institute of Pharmacology & Toxicology
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.
Sun Yat-Sen University
Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease.
Sun Yat-Sen University
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
Duke University Medical Center
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
Sun Yat-Sen University
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.
Sichuan University/Collaborative Innovation Center of Biotherapy
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.
Duke University Medical Center
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.
Wuxi Apptec (Shanghai) Co.
Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.
Amgen
Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors.
Shanghai Institute of Pharmaceutical Industry
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.
University of Pennsylvania
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Sichuan University and Collaborative Innovation Center
QUINOLINE MERCAPTOACETATE SULFONAMIDE DERIVATIVE, INTERMEDIATE, PHARMACEUTICAL DERIVATIVE OR FORMULATION, AND PREPARATION METHOD AND USE THEREFOR
JIANGSU CHIATAI QINGJIANG PHARMACEUTICAL CO., LTD.
SERIES OF PIPERIDINE-SUBSTITUTED BENZOIC ACID COMPOUNDS, AND USE THEREOF
Medshine Discovery
Modulators of Cystic Fibrosis Transmembrane Conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulators
Vertex Pharmaceuticals
3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
Board of Trustees of The Southern Illinois University
Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors
Xenon Pharmaceuticals
Biphenyl-ethyl-pyrrolidine derivatives as histamine H3 receptor modulators for the treatment of cognitive disorders
Arena Pharmaceuticals
Pyrazole and imidazole derivatives useful as orexin antagonists
Actelion Pharmaceuticals
NAD+-dependent DNA ligase (Rv3014c) from M. tuberculosis: Strategies for inhibitor design
Central Drug Research Institute