141 articles for L Huang
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
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Data
Article Title
Organization
4
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Amgen
5
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
10
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.
Peking Union Medical College
27
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
Huazhong University of Science and Technology
14
Synthesis and evaluation of selegiline derivatives as monoamine oxidase inhibitor, antioxidant and metal chelator against Alzheimer's disease.
Sun Yat-Sen University
10
Discovery of novel non-covalent inhibitors selective to the 5-subunit of the human 20S proteasome.
Peking Union Medical College
4
Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.
University of Pennsylvania
13
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
University of Pennsylvania
48
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
China Pharmaceutical University
14
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
2
Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
6
Design, synthesis and evaluation of dual pharmacology 2-adrenoceptor agonists and PDE4 inhibitors.
Sun Yat-Sen University
3
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Amgen
11
Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity.
Sun Yat-Sen University
19
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
Sun Yat-Sen University
18
Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen.
Sun Yat-Sen University
15
Synthesis and biological evaluation of berberine-thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and A aggregation and antioxidant activity.
Sun Yat-Sen University
3
Design, synthesis, and evaluation of multitarget-directed resveratrol derivatives for the treatment of Alzheimer's disease.
Sun Yat-Sen University
5
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
16
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
11
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
1
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
11
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
20
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
21
Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.
Sun Yat-Sen University
2
Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes.
Sichuan University
20
Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids.
Sun Yat-Sen University
41
The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.
Amgen
44
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
Amgen
14
Design, synthesis, and biological evaluation of semicarbazide-sensitive amine oxidase (SSAO) inhibitors with anti-inflammatory activity.
La Jolla Pharmaceutical
2
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.
University of North Carolina
13
Dualß2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
Sun Yat-Sen University
26
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Amgen
16
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
Guangzhou Institute of Biomedicine and Health
26
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
15
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
39
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
86
Discovery and SAR of methylated tetrahydropyranyl derivatives as inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT).
Myrexis
28
Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4.
University of Pennsylvania
18
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors.
Sun Yat-Sen University
13
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.
Sun Yat-Sen University
30
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
Sun Yat-Sen University
10
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.
Shanghai Hengrui Pharmaceuticals
17
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
Sun Yat-Sen University
5
Zaragozic Acids D and D2: Potent Inhibitors of Squalene Synthase and of Ras Farnesyl-Protein Transferase
TBA
25
Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
Amgen
20
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Amgen
26
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
18
Discovery of High-Affinity SMARCA2/4 Bromodomain Ligands and Development of Potent and Exceptionally Selective SMARCA2 PROTAC Degraders.
University of Michigan
32
Discovery of novel tranylcypromine-indazole-based derivatives as LSD1 inhibitors for acute myeloid leukemia treatment.
Zhengzhou University
40
Discovery and Optimization of Novel Apo-IDO1 Inhibitors by a Pharmacophore-Based Structural Simplification Strategy.
China Pharmaceutical University
3
Design, synthesis and structure-activity relationship of novel 1,2,4-triazolopyrimidin-5-one derivatives targeting GABAA1 and Nav1.2 with antiepileptic activity.
Qingdao University of Science and Technology
3
Development of a Highly Selective Ferroptosis Inducer Targeting GPX4 with 2-Ethynylthiazole-4-carboxamide as Electrophilic Warhead.
Hainan University
93
Discovery of FHD-286, a First-in-Class, Orally Bioavailable, Allosteric Dual Inhibitor of the Brahma Homologue (BRM) and Brahma-Related Gene 1 (BRG1) ATPase Activity for the Treatment of SWItch/Sucrose Non-Fermentable (SWI/SNF) Dependent Cancers.
Foghorn Therapeutics
6
Discovery of SMD-3236: A Potent, Highly Selective and Efficacious SMARCA2 Degrader for the Treatment of SMARC4-Deficient Human Cancers.
University of Michigan
25
Discovery of Potent, Highly Selective, and Efficacious SMARCA2 Degraders.
SK Life Science Labs
26
Discovery of a novel KV7.2/7.3 channels agonist for the treatment of neuropathic pain.
Jiangsu Ocean University
13
The Potential of PARP Inhibitors as Antitumor Drugs and the Perspective of Molecular Design.
Qingdao University of Science and Technology
5
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.
Xiamen University
3
Design, synthesis and biological evaluation of novel DCLK1 inhibitor containing purine skeleton for the treatment of pancreatic cancer.
China Pharmaceutical University
3
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.
Ocean University of China
36
Discovery of Imidazo[1,2-a]pyrazine Derivatives as Potent ENPP1 Inhibitors.
Shanghai Institute of Materia Medica
4
Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment.
China Pharmaceutical University
2
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
1
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
2
Dual Antagonism of α9α10 nAChR and GABAB Receptor-Coupled CaV2.2 Channels by an Analgesic αO-Conotoxin Analogue.
Ocean University of China
50
Design, Synthesis, and Evaluation of the Selective and Orally Active LSD1 Inhibitor with the Potential of Treating Heart Failure.
Zhengzhou University
25
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
China Pharmaceutical University
23
Heterocyclic-Modified Imidazoquinoline Derivatives: Selective TLR7 Agonist Regulates Tumor Microenvironment against Melanoma.
Southern Medical University
8
Novel small molecule inhibitors targeting renal cell carcinoma: Status, challenges, future directions.
Sichuan University
4
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors.
Sichuan University
3
Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong
University of Michigan
13
Discovery of the Potent and Highly Selective PARP7 Inhibitor as a Novel Immunotherapeutic Agent for Tumors.
China Pharmaceutical University
3
The importance of indole and azaindole scaffold in the development of antitumor agents.
Qingdao University of Science and Technology
10
Discovery of the First Selective IDO2 Inhibitor As Novel Immunotherapeutic Avenues for Rheumatoid Arthritis.
China Pharmaceutical University
50
Identification of N, C-capped di- and tripeptides as selective immunoproteasome inhibitors.
Peking Union Medical College
12
Novel non-benzimidazole chk2 kinase inhibitors.
Johnson and Johnson Pharmaceutical Research and Development
8
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.
Nanjing University
11
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
Shanghai Institute of Technology
1
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
Peking Union Medical College
47
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
Johnson & Johnson Pharmaceutical Research and Development
19
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.
China Pharmaceutical University
20
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
10
Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype.
Bristol Myers Squibb
25
Discovery and Evaluation of Pyrazolo[3,4-
Hubei Bio-Pharmaceutical Industrial Technological Institute
19
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
Jiangsu Ocean University
13
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.
University Of California
38
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
40
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
University Of California
31
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Merck
14
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
38
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6
Harvard Medical School
17
Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
Sun Yat-Sen University
30
Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Guangzhou University of Chinese Medicine
5
A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45.
Ningbo University
14
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
26
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
11
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
30
Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.
Toho University
43
Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.
TBA
1
TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.
East China Normal University
40
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
15
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong
TBA
2
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
6
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
20
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
16
Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease.
Sun Yat-Sen University
2
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
Duke University Medical Center
19
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
Sun Yat-Sen University
34
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
1
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.
Duke University Medical Center
17
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.
Wuxi Apptec (Shanghai) Co.
170
Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.
Amgen
23
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
7
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.
University of Pennsylvania
10
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Sichuan University and Collaborative Innovation Center
8
QUINOLINE MERCAPTOACETATE SULFONAMIDE DERIVATIVE, INTERMEDIATE, PHARMACEUTICAL DERIVATIVE OR FORMULATION, AND PREPARATION METHOD AND USE THEREFOR
JIANGSU CHIATAI QINGJIANG PHARMACEUTICAL CO., LTD.
4
SERIES OF PIPERIDINE-SUBSTITUTED BENZOIC ACID COMPOUNDS, AND USE THEREOF
Medshine Discovery
210
Modulators of Cystic Fibrosis Transmembrane Conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulators
Vertex Pharmaceuticals
71
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
62
Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors
Xenon Pharmaceuticals
26
Biphenyl-ethyl-pyrrolidine derivatives as histamine H3 receptor modulators for the treatment of cognitive disorders
Arena Pharmaceuticals
145
Pyrazole and imidazole derivatives useful as orexin antagonists
Actelion Pharmaceuticals
6
NAD+-dependent DNA ligase (Rv3014c) from M. tuberculosis: Strategies for inhibitor design
Central Drug Research Institute