165 articles for Y Yu
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
22
Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.
Sun Yat-Sen University
43
N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.
Boehringer Ingelheim Pharmaceuticals
11
Eucarobustols A-I, Conjugates of Sesquiterpenoids and Acylphloroglucinols from Eucalyptus robusta.
Chinese Academy of Sciences
6
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.
Southern Medical University
11
6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR.
Zhejiang University
8
Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors.
Sookmyung Women'S University
34
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.
Merck Research Laboratories
19
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.
Merck Research Laboratories
42
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
31
Synthesis and biological evaluations of novel endomorphin analogues containinga-hydroxy- -phenylalanine (AHPBA) displaying mixedµ/d opioid receptor agonist andd opioid receptor antagonist activities.
Zhejiang University
32
Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors.
Liaoning Normal University
25
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
6
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.
Merck Research Laboratories
44
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
Merck Research Laboratories
24
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Merck Research Laboratories
29
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Merck Research Laboratories
5
Reaction intermediate analogues as bisubstrate inhibitors of pantothenate synthetase.
Soochow University
27
Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.
Torrey Pines Institute For Molecular Studies
2
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.
Zhejiang University
21
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.
Merck Research Laboratories
6
Synthesis and biological evaluation of oleanolic acid derivatives as PTP1B inhibitors.
North-West University
22
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
AstraZeneca
52
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
AstraZeneca
22
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Pfizer
33
1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Pfizer
15
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Schering-Plough Research Institute
33
Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNFa-induced nuclear factor-¿B activation inhibition.
Sun Yat-Sen University
11
Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors.
Wenzhou Medical College
4
Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents.
Zhejiang University
45
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Pfizer
37
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.
AstraZeneca
14
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
Pfizer
47
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Pfizer
33
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
Pfizer
34
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Schering-Plough Research Institute
2
Discovery of a novel protein kinase B inhibitor by structure-based virtual screening.
Torrey Pines Institute For Molecular Studies
6
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.
Pfizer
23
3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.
Schering-Plough Research Institute
22
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
Schering-Plough Research Institute
75
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
AstraZeneca
8
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Lanzhou University
1
2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents.
Zhejiang University
43
Identification of Oral Bioavailable Coumarin Derivatives as Potential AR Antagonists Targeting Prostate Cancer.
Zhejiang University
9
Design, synthesis, and biological evaluation of Ponatinib-based N-Phenylpyrimidine-2-amine derivatives as novel fibroblast growth factor receptor 4 (FGFR4) selective inhibitors.
Chongqing Medical University
49
Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor.
Abbvie, Inc
12
Optimization of SHP2 allosteric inhibitors with novel tail heterocycles and their potential as antitumor therapeutics.
Shandong University
3
A Prostate-Specific Membrane Antigen-Targeting Small Molecule-Drug Conjugate Strategy to Overcome the Hematological Toxicity of Olaparib.
Zhejiang University
32
Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors.
Merck & Co.
1
211At radiolabeled APBA-FAPI for enhanced targeted-alpha therapy of glioma.
Sichuan University
41
Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.
Schering-Plough Research Institute
6
Design and synthesis of 7-membered lactam fused hydroxypyridinones as potent metal binding pharmacophores (MBPs) for inhibiting influenza virus PAN endonuclease.
Zhejiang University
10
Investigating Active Site Binding of Ligands to High and Low Activity Carbonic Anhydrase Enzymes Using Native Mass Spectrometry.
Griffith University
1
Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy.
Tongji University
21
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
Schering-Plough Research Institute
8
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
20
Design, Synthesis and Antitumor Activity of a Novel Class of SHP2 Allosteric Inhibitors with a Furanyl Amide-Based Scaffold.
Shandong University
6
Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit.
Zhejiang University
91
Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis.
Zhejiang University
74
Novel Benzo Five-Membered Heterocycle Derivatives as P-Glycoprotein Inhibitors: Design, Synthesis, Molecular Docking, and Anti-Multidrug Resistance Activity.
Zhejiang University
13
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
1
Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer.
Icahn School Of Medicine At Mount Sinai
27
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Johnson & Johnson Pharmaceutical Research & Development
20
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
Schering-Plough Research Institute
30
Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.
East China Normal University
1
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
Johnson & Johnson Pharmaceutical Research & Development
15
Development and Characterization of Fluorescent Probes for the G Protein-Coupled Receptor 35.
Dalian Institute of Chemical Physics
2
The discovery of cyclic γ-AApeptides as the promising ligands targeting EP2.
University of South Florida
24
Accelerated Discovery of Macrocyclic CDK2 Inhibitor QR-6401 by Generative Models and Structure-Based Drug Design.
Tencent Ai Lab
8
Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery.
China Pharmaceutical University
2
EP2 Antagonists (2011-2021): A Decade's Journey from Discovery to Therapeutics.
University of Tennessee Health Science Center
54
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
Merck
13
Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein-Protein Interactions between DOT1L and MLL-AF9/MLL-ENL.
China Pharmaceutical University
18
Design, Synthesis, and Proof-of-Concept of Triple-Site Inhibitors against Aminoacyl-tRNA Synthetases.
Sun Yat-Sen University
42
Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α.
Merck
30
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
Washington University
15
Synthesis and activity evaluation of selenazole-coupled CPI-1 irreversible bifunctional inhibitors for botulinum toxin A light chain.
Guizhou Medical University
15
Optimization of Beclin 1-Targeting Stapled Peptides by Staple Scanning Leads to Enhanced Antiproliferative Potency in Cancer Cells.
Fudan University
25
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
Merck
27
Discovery of the First Non-cGMP Mimetic Small Molecule Activators of cGMP-Dependent Protein Kinase 1 α (PKG1α).
Merck
11
Discovery of a Potent and Orally Bioavailable Hypoxia-Inducible Factor 2α (HIF-2α) Agonist and Its Synergistic Therapy with Prolyl Hydroxylase Inhibitors for the Treatment of Renal Anemia.
China Pharmaceutical University
23
Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.
X-Chem
6
Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
Chongqing Medical University
32
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.
Merck
27
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Merck
38
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Merck Research Laboratories
3
Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities.
Chongqing Medical University
20
Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.
Washington University School of Medicine
4
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Xihua University
19
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Merck
36
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Merck
3
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.
Ocean University of China
53
Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents.
Pfizer
3
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
Sun Yat-Sen University
6
Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants.
Zhejiang University
53
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Merck
4
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
Chongqing Medical University
35
Structure-Based Development of (1-(3'-Mercaptopropanamido)methyl)boronic Acid Derived Broad-Spectrum, Dual-Action Inhibitors of Metallo- and Serine-β-lactamases.
Sichuan University
2
Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light.
China Pharmaceutical University
25
Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity.
Zhejiang University
19
Design, Synthesis, and Biological Evaluation of Imidazo[1,2-
East China Normal University
96
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents.
Searle Research and Development
42
1,2-Diarylpyrroles as potent and selective inhibitors of cyclooxygenase-2.
Searle Research and Development
6
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.
Merck
22
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
AstraZeneca
3
Synthesis and identification of new 4-arylidene curcumin analogues as potential anticancer agents targeting nuclear factor-κB signaling pathway.
Sun Yat-Sen University
28
Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
Wuhan University
40
X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.
West China School of Pharmacy
36
Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors.
Southern Medical University
2
Bioactive Asarone-Derived Phenylpropanoids from the Rhizome of Acorus tatarinowii Schott.
College of Pharmacy/Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Tcm and New Drugs Research
2
Design, synthesis and structure-activity relationship studies of a focused library of pyrimidine moiety with anti-proliferative and anti-metastasis activities in triple negative breast cancer.
Shenyang Pharmaceutical University
23
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Merck
50
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Merck
31
Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.
AstraZeneca
47
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Merck
26
Highly Selective and Potentα4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.
Torrey Pines Institute For Molecular Studies
33
INHIBITORS OF ANTIMOCROBIAL RESISTANCE AND METHOS USING SAME
Baylor College of Medicine
45
AZETIDINE DERIVATIVES AND USE THEREOF AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS
Chiesi Farmaceutici
7
FAK DEGRADERS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC APPLICATIONS
Berrybio (Shanghai)
4
METHIONINE ADENOSYLTRANSFERASE 2A HETEROCYCLIC INHIBITOR
Nanjing Chia Tai Tianqing Pharmaceutical Co.
29
HETEROBIVALENT AND HOMOBIVALENT AGENTS TARGETING FIBROBLAST ACTIVATION PROTEIN ALPHA AND/OR PROSTATE-SPECIFIC MEMBRANE ANTIGEN
The Johns Hopkins University
14
MODULATORS OF A POTASSIUM CHANNEL AND OF TRPV1 CHANNEL AND USES THEREOF
Bsense Bio Therapeutics
108
3-[(1H-PYRAZOL-R-YL)OXY]PYRAZIN-2-AMINE COMPOUNDS AS HPK1 INHIBITOR AND USE THEREOF
Beigene
8
BIVALENT LIGANDS TO UNDERSTAND DIMERIZATION OF THE MU OPIOID RECEPTOR AND THE CHEMOKINE RECEPTOR CCR5 IN NEUROLOGICAL DISORDERS
Virginia Commonwealth University
2
ORALLY BIOAVAILABLE, BRAIN-PENETRANT COMPOUND WITH SELECTIVITY FOR THE CANNABINOID TYPE 2 RECEPTOR WITH POTENTIAL USE TOWARDS VISCERAL PAIN MANAGEMENT AND NEURODEGENERATIVE DISORDERS
University of Mississippi
289
3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives
GrÜNenthal
32
Six-membered ring benzo derivatives as DPP-4 inhibitor and use thereof
East China University of Science and Technology
815
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma
15
3-(indolyl)- or 3-(azaindolyl)- 4-arylmaleimide derivatives for use in the treatment of colon and gastric adenocarcinoma
Johannes Gutenberg-UniversitäT Mainz
39
Benzodioxole derivative and preparation method and use thereof
Zhejiang Hisun Pharmaceutical
1
Structural basis for the recognition of mycolic acid precursors by KasA, a condensing enzyme and drug target from Mycobacterium tuberculosis.
University of Wuerzburg
198
Benzylamine derivatives as inhibitors of plasma kallikrein
Kalvista Pharmaceuticals
8
Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2
Sapienza University of Rome
8
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Merck Sharpe & Dohme
7
Identification of exosite-targeting inhibitors of anthrax lethal factor by high-throughput screening.
Yale University
1
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Abbott Laboratories
5
COMPOUNDS, COMPOSITIONS, AND METHODS FOR REDUCING PRODUCTION OF TRIMETHYLAMINE
The Cleveland Clinic Foundation