146 articles for M Liu
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Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
East China University of Science and Technology
Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking.
The Ohio State University
GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved
Genentech
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)
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
Merck Research Laboratories
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
Pharmaron-Beijing
Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.
Acelot
Discovery of novel spiro 1,3,4-thiadiazolines as potent, orally bioavailable and brain penetrant KSP inhibitors.
Merck Research Laboratories
Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors.
Vertex Pharmaceuticals
Identification of indole-3-carboxylic acids as non-ATP-competitive Polo-like kinase 1 (Plk1) inhibitors.
China Pharmaceutical University
Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Identification of novel HSP90a/ß isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Vertex Pharmaceuticals
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Bristol-Myers Squibb Research and Development
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).
The Institute of Cancer Research
Correlation between chemotype-dependent binding conformations of HSP90a/ß and isoform selectivity-Implications for the structure-based design of HSP90a/ß selective inhibitors for treating neurodegenerative diseases.
Vertex Pharmaceuticals
Tacrine-ferulic acid-nitric oxide (NO) donor trihybrids as potent, multifunctional acetyl- and butyrylcholinesterase inhibitors.
China Pharmaceutical University
Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.
Hoffmann-La Roche
Cucurbitane glucosides from the root of Machilus yaoshansis.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine
Structural investigation into the inhibitory mechanisms of indomethacin and its analogues towards human glyoxalase I.
Sun Yat-Sen University
Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.
Harvard Medical School
Biological study of a somatostatin mimetic based on the 1-deoxynojrimycin scaffold.
Shandong University School of Medicine
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
Design, synthesis and biological evaluation of 4-(4-aminophenoxy)picolinamide derivatives as potential antitumor agents.
The First Affiliated Hospital of Wenzhou Medical University
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death.
Shandong University
Discovery of pyridazinone derivatives bearing tetrahydroimidazo[1,2-a]pyrazine scaffold as potent inhibitors of transient receptor potential canonical 5 to ameliorate hypertension-induced renal injury in rats.
Nanjing University of Chinese Medicine
Unleashing the Potential of Camptothecin: Exploring Innovative Strategies for Structural Modification and Therapeutic Advancements.
Southwest Jiaotong University
Design, Synthesis, and Activity Evaluation of Novel Benzazole Bifunctional Antifungal Inhibitors with an LDH Carrier.
Liaocheng University
Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins.
Sichuan University
Structure-Guided Discovery of Potent and Selective CLK2 Inhibitors for the Treatment of Knee Osteoarthritis.
China Pharmaceutical University
Research progress of DDR1 inhibitors in the treatment of multiple human diseases.
Sichuan University
Discovery of Anti-SARS-CoV-2 Nsp9 Binders from Natural Products by a Native Mass Spectrometry Approach.
Griffith University
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.
Sichuan University
Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
Shandong University
Optimization, and biological evaluation of 3-O-β-chacotriosyl betulinic acid amide derivatives as novel small-molecule Omicron.
South China Agricultural University
Construction and Evaluation of Novel Dual-function Antifungal Inhibitors and Covalent Organic Framework Carriers Based on the Infection Microenvironment.
Liaocheng University
Design, Synthesis, and Activity Evaluation of Novel Dual-Target Inhibitors with Antifungal and Immunoregulatory Properties.
Liaocheng University
Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer.
East China Normal University
Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.
Shenyang Pharmaceutical University
Discovery of quinazolin-4-one-based non-covalent inhibitors targeting the severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2 M
China Pharmaceutical University
Recent researches for dual Aurora target inhibitors in antitumor field.
Chengdu University
Drugs for the treatment of glaucoma: Targets, structure-activity relationships and clinical research.
Chengdu Sport University
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Abbott Laboratories
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Abbott Laboratories
Design, Synthesis, and Bioevaluation of Pyrido[2,3-
Nanjing University of Chinese Medicine
Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation.
Liaocheng University
Scaffold Hopping Strategy to Identify Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy.
East China Normal University
Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease
Anhui Medical University
Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis.
East China Normal University
Optimization of NAMPT activators to achieve in vivo neuroprotective efficacy.
School of Pharmaceutical Sciences
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Abbott Laboratories
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
Shenyang Pharmaceutical University
Discovery of pyrroledione analogs as potent transient receptor potential canonical channel 5 inhibitors.
China Pharmaceutical University
Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.
Peking Union Medical College
Discovery and optimization of new 6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline derivatives as potent influenza virus PA
South China Agricultural University
Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
East China Normal University
Synthesis of AC1903 analogs as potent transient receptor potential canonical channel 4/5 inhibitors and biological evaluation.
Chinese Academy of Sciences
NAE modulators: A potential therapy for gastric carcinoma.
Southwest Jiaotong University
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
Shandong University
Design, Synthesis, and Biological Evaluation of Dual-Target COX-2/CYP51 Inhibitors for the Treatment of Fungal Infectious Diseases.
Liaocheng University
Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
Shenyang Pharmaceutical University
Identification, optimization, and biological evaluation of 3-O-β-chacotriosyl ursolic acid derivatives as novel SARS-CoV-2 entry inhibitors by targeting the prefusion state of spike protein.
South China Agricultural University
Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr
East China Normal University
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
University of Science and Technology of China
Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.
East China Normal University
Identification of (6S)-cyclopropyl-6,7-dihydropyrazolo[1,5-a]pyrazine-5(4H)-carboxamines as new HBV capsid assembly modulators.
Cams Key Laboratory of Antiviral Drug Research
Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery.
Peking University Shenzhen Graduate School
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
Shandong University
Identification of 3, 4-disubstituted pyridine derivatives as novel CDK8 inhibitors.
Peking Union Medical College
Discovery and structural optimization of 3-O-β-chacotriosyl oleanane-type triterpenoids as potent entry inhibitors of SARS-CoV-2 virus infections.
South China Agricultural University
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
East China Normal University
Novel naphthylamide derivatives as dual-target antifungal inhibitors: Design, synthesis and biological evaluation.
Liaocheng University
Effects of C-Terminal B-Chain Modifications in a Relaxin 3 Agonist Analogue.
University of Melbourne
Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.
Schering-Plough Research Institute
Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.
Fondazione Istituto Italiano Di Tecnologia
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist.
Zhejiang Normal University
Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.
Cancer Research Uk Cancer Therapeutics Unit
Discovery of coumarin-based selective aldehyde dehydrogenase 1A1 inhibitors with glucose metabolism improving activity.
China Pharmaceutical University
Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y4 Receptor Agonist Derived by an Olefin Metathesis Approach.
Monash University (Parkville Campus)
Bipolaricins A-I, Ophiobolin-Type Tetracyclic Sesterterpenes from a Phytopathogenic
Huazhong University of Science and Technology
Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R.
Monash University (Parkville Campus)
Small-Molecule Antagonist Targeting Exportin-1 via Rational Structure-Based Discovery.
Dalian University of Technology
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.
Georgetown University Medical Center
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Schering-Plough Research Institute
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Merck
Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.
Southern Medical University
Synthesis and Biological Evaluation of B-Cell Lymphoma 6 Inhibitors of
East China Normal University and Shanghai Fengxian District Central Hospital Joint Center For Translational Medicine
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
Peking Union Medical College
Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis.
Anhui Medical University
Synthesis of urea analogues bearing N-alkyl-N'-(thiophen-2-yl) scaffold and evaluation of their innate immune response to toll-like receptors.
Southern Medical University
Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors.
University of Illinois At Chicago
Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.
Schering-Plough Research Institute
Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.
Schering-Plough Research Institute
Monosaccharide Analogues of Anticancer Peptide R-Lycosin-I: Role of Monosaccharide Conjugation in Complexation and the Potential of Lung Cancer Targeting and Therapy.
TBA
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compounds.
Schering-Plough Research Institute
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
University of South China
Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
Shandong University
New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.
Merck Research Laboratories
Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: potent allosteric inhibitors of the hepatitis C virus NS5B polymerase.
Bristol-Myers Squibb
Modification and Biological Evaluation of a Series of 1,5-Diaryl-1,2,4-triazole Compounds as Novel Agents against Pancreatic Cancer Metastasis through Targeting Myoferlin.
East China Normal University
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Merck Research Laboratories
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
Merck Research Laboratories
Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PA
South China Agricultural University
Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives.
Peking Union Medical College
Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
East China Normal University
Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B.
Shenyang Pharmaceutical University
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Merck
BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.
Huazhong University of Science and Technology
Design, semisynthesis, α-glucosidase inhibitory, cytotoxic, and antibacterial activities of p-terphenyl derivatives.
Ocean University of China
Discovery of BMS-961955, an allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Bristol-Myers Squibb Research and Development
Improving Metabolic Stability with Deuterium: The Discovery of BMT-052, a Pan-genotypic HCV NS5B Polymerase Inhibitor.
Bristol-Myers Squibb Research and Development
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity.
Shenyang Pharmaceutical University
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Bristol-Myers Squibb Research and Development
AZETIDINE DERIVATIVES AND USE THEREOF AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS
Chiesi Farmaceutici
PYRAZOLE COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF
Sichuan Kelun-Biotech Biopharmaceutical
2-oxo-6,7-dihydrobenzo[a]quinolizine-3-carboxylic acid derivatives for the treatment and prophylaxis of hepatitis B virus infection
Hoffmann-La Roche
Synthesis of novel disulfide and sulfone hybrid scaffolds as potent ß-glucuronidase inhibitor.
Universiti Teknologi Mara
Novel inhibitors of human DOPA decarboxylase extracted from Euonymus glabra Roxb.
Shanghai Center For Systems Biomedicine
Screening and X-ray crystal structure-based optimization of autotaxin (ENPP2) inhibitors, using a newly developed fluorescence probe.
The University of Tokyo
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases.
Universidad San Pablo Ceu
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.
Bristol-Myers Squibb