168 articles for L Xu
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Article Title
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Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Merck
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect isletβ-cells from apoptosis.
East China Normal University
Phloroglucinol Derivatives with Protein Tyrosine Phosphatase 1B Inhibitory Activities from Eugenia jambolana Seeds.
Northeastern University
Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
South China University of Technology
The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics.
Merck
Design, synthesis and biological evaluation of novel non-covalent piperidine-containing peptidyl proteasome inhibitors.
Hangzhou Xixi Hospital
Discovery of a novel 6,7-disubstituted-4-(2-fluorophenoxy)quinolines bearing 1,2,3-triazole-4-carboxamide moiety as potent c-Met kinase inhibitors.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.
University of Kansas
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
Zhejiang University
Design and optimization of tricyclic gamma-secretase modulators.
Bristol-Myers Squibb Research and Development
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.
Fudan University
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.
Zhejiang University
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase.
East China University of Science and Techology
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.
Zhejiang University
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed fromß-amino acid as proteasome inhibitors.
Zhejiang University
Discovery of novel inhibitors targeting the macrophage migration inhibitory factor via structure-based virtual screening and bioassays.
Zhejiang University
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.
Merck
The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.
Merck
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350).
Gilead Sciences
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: core region.
Gilead Sciences
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Merck Research Laboratories
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Merck Frosst Centre For Therapeutic Research
Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable ¿-Secretase Modulator.
TBA
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.
Chinese Academy of Sciences
Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase.
The Scripps Research Institute
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).
Fudan University
Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives.
University of New Orleans
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
University of Michigan Comprehensive Cancer Center
Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
University of New Orleans
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives.
University of New Orleans
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
Celgene
Discovery of 4-aminomethylphenylacetic acids as¿-secretase modulators via a scaffold design approach.
Biogen Idec
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.
Zhejiang University
A sucrose-derived scaffold for multimerization of bioactive peptides.
The University of Arizona
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Merck
Design, synthesis, and biological studies of efficient multivalent melanotropin ligands: tools toward melanoma diagnosis and treatment.
Pierre and Marie Curie University
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.
Merck Research Laboratories
Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.
Merck Frosst Center For Therapeutic Research
Efficient synthesis and biological evaluation of epiceanothic acid and related compounds.
China Pharmaceutical University
Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.
Southeast University
Synthesis and biological evaluation of 5,6-diarylimidazo[2.1-b]thiazole as selective COX-2 inhibitors
TBA
Synthesis and biological evaluation of 2,3-diarylthiophenes as selective cox-2 inhibitors. part II: Replacing the heterocycle
TBA
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma a
Merck Research Laboratories
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
Merck Research Laboratories
Isolation and structure elucidation of Sch 642305, a novel bacterial DNA primase inhibitor produced by Penicillium verrucosum.
Schering-Plough Research Institute
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists.
Nanjing University of Chinese Medicine
Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy.
Hangzhou Normal University
Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione.
Bristol Myers Squibb
Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells.
Shanghai Jiao Tong University
Identification of 3-aryl-5-methyl-isoxazole-4-carboxamide derivatives and analogs as novel HIF-2α agonists through docking-based virtual screening and structural modification.
Zhejiang University
Discovery of Novel Inhibitors of BRD4 for Treating Prostate Cancer: A Comprehensive Case Study for Considering Water Networks in Virtual Screening and Drug Design.
Zhejiang 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 Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
Shanghai Institute of Materia Medica
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor.
Nankai University
Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity.
Wuyi University
Benzothiazole derivatives as histone deacetylase inhibitors for the treatment of autosomal dominant polycystic kidney disease.
Xuzhou Medical University
Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway.
Ningxia Medical University
Recent advances in EZH2-based dual inhibitors in the treatment of cancers.
Xinxiang University
Rational Design of Sulfonyl-γ-AApeptides as Highly Potent HIV-1 Fusion Inhibitors with Broad-Spectrum Activity.
University of South Florida
Discovery and Optimization of a STING Agonist Platform for Application in Antibody Drug Conjugates.
Mersana Therapeutics
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.
Zhejiang University
Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7.
Shanghaitech University
Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations.
Jiangnan University
Tetracyclic Steroids Bearing a Bicyclo[4.4.1] Ring System as Potent Antiosteoporosis Agents from the Deep-Sea-Derived Fungus
Third Institute of Oceanography
Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors.
Soochow University
Crystallography-Guided Optimizations of the Keap1-Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides.
Ningxia Medical University
Medicinal chemistry updates of novel HDACs inhibitors (2020 to present).
Hangzhou Normal 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 a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
Merck Research Laboratories
Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.
China Pharmaceutical University
Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors.
The Scripps Research Institute
Identification of novel influenza polymerase PB2 inhibitors using virtual screening approach and molecular dynamics simulation analysis of active compounds.
Beijing Institute of Pharmacology and Toxicology
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Discovery of highly potent and selective EGFR
Beijing Institute of Pharmacology and Toxicology
Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin-3 Inhibitors.
Bristol Myers Squibb
Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors.
China Pharmaceutical University
Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings.
Emory University
Development of peptide epoxyketones as selective immunoproteasome inhibitors.
Zhejiang University
The development of potent non-peptidic PTP-1B inhibitors.
Merck Frosst Centre For Therapeutic Research
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
Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.
Ningxia Medical University
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.
Chinese Academy of Sciences
Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor.
Ningxia Medical University
Discovery of Selective Small-Molecule Inhibitors for the ENL YEATS Domain.
Texas A&M University
Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H
Xuzhou Medical University
Multifunctional agents based on benzoxazolone as promising therapeutic drugs for diabetic nephropathy.
Beijing Institute of Technology
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.
Abbott Laboratories
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.
Merck Frosst Centre For Therapeutic Research
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Merck And
Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Bristol-Myers Squibb
Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.
Zhejiang University
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models.
Chinese Academy of Sciences
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.
Hangzhou Xixi Hospital
Design, synthesis and biological evaluation of novel pteridinone derivatives possessing a hydrazone moiety as potent PLK1 inhibitors.
Shenyang Pharmaceutical University
Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors.
Jiangnan University
Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.
Merck Research Laboratories
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.
Hangzhou Institute of Innovative Medicine
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.
Zhejiang University
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Chinese Academy of Sciences
-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[
Ningxia Medical University
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
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
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Abbott Laboratories
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.
Zhejiang University
Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Zhejiang University
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.
Shenyang Pharmaceutical University
Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
Ningxia Medical University
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.
Abbott Laboratories
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.
Zhejiang University
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.
Zhejiang University
Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors.
Yanbian University
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.
Hangzhou Institute of Innovative Medicine
Synthesis and evaluation of cholecystokinin trimers: a multivalent approach to pancreatic cancer detection and treatment.
Pierre and Marie Curie University
Development of Unsymmetrical Dyads As Potent Noncarbohydrate-Based Inhibitors against Human β-N-Acetyl-d-hexosaminidase.
East China University of Science and Technology
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.
Merck Research Laboratories
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 7- and 5-, 6-, 8-positions.
Maxim Pharmaceuticals
Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation.
China Pharmaceutical University
Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces.
Chinese Academy of Sciences
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.
Chinese Academy of Sciences
Quinoline hybrids and their antiplasmodial and antimalarial activities.
Hubei Engineering University
Benzo[c][1,2,5]thiadiazole derivatives: A new class of potent Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors.
Jiangnan University
High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex.
Nanjing Forestry University
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.
Chinese Academy of Sciences
Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
Dalian Medical University
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.
Novartis Institutes For Biomedical Research
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.
Merck
COXIB-DERIVED CONJUGATE COMPOUNDS AND METHODS OF USE THEREOF
Reiley Pharmaceuticals
ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY
Merck Sharp & Dohme
BACTERIAL DNA GYRASE INHIBITORS AND METHODS OF USE THEREOF
The Florida International University Board of Trustees
Substituted pyrazlo[3,4-c]pyridines as selective BTK kinase inhibitors
Jumbo Drug Bank
Benzene disulfonamide for the treatment of cancer
Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Boehringer Ingelheim International
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.
Pfizer
Inhibition of AcpA phosphatase activity with ascorbate attenuates Francisella tularensis intramacrophage survival.
University of Florida
Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells.
Universit&Aagrove
[125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors.
U. 109
Solvent and guest isotope effects on complexation thermodynamics of alpha-, beta-, and 6-amino-6-deoxy-beta-cyclodextrins.
Japan Science and Technology Agency