107 articles for thisTarget
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Protective effect of novel substituted nicotine hydrazide analogues against hypoxic brain injury in neonatal rats via inhibition of caspase.
The Fifth Affiliated Hospital of Guangzhou Medical University
Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) Ministry of Education
In vitro induction of apoptosis by isosclerone from marine-derived fungus Aspergillus fumigatus.
Pukyong National University
Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.
TBA
Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis.
Westf£Lische Wilhelms-Universit£T M£Nster
1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.
Tianjin University of Science and Technology
Influence of 4- or 5-substituents on the pyrrolidine ring of 5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin derivatives on their inhibitory activities towards caspases-3 and -7.
Westf£Lische Wilhelms-Universit£T M£Nster
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.
Nankai University
Synthesis, 18F-radiolabeling, and in vivo biodistribution studies of N-fluorohydroxybutyl isatin sulfonamides using positron emission tomography.
Westf£Lische Wilhelms-Universit£T M£Nster
Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: nonradioactive counterparts of putative PET-compatible apoptosis imaging agents.
Westf£Lische Wilhelms-Universit£T M£Nster
New description of protein-ligand interactions using a spherical self-organizing map.
Chugai Pharmaceutical
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease.
Evotec (Uk)
A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions.
Southern Medical University
Caspase-1 and -3 inhibiting drimane sesquiterpenoids from the extremophilic fungus Penicillium solitum.
University of Montana
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.
Procter and Gamble Pharmaceuticals
Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis.
Procter & Gamble Pharmaceuticals
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Maxim Pharmaceuticals
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).
Institute For Drug Research
Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors.
Chdi Management
Aspartic vinyl sulfones: inhibitors of a caspase-3-dependent pathway.
University of Lisbon
Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.
Washington University
Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study.
University of Lisbon
Mechanisms, biology and inhibitors of deubiquitinating enzymes.
Institute For Bio-Medical Research
Design, synthesis, and discovery of novel non-peptide inhibitor of Caspase-3 using ligand based and structure based virtual screening approach.
Osmania University College For Women
Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis.
Westfalische Wilhelms-Universitat
Fluorinated isatin derivatives. Part 1: synthesis of new N-substituted (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatins as potent caspase-3 and -7 inhibitors.
WestfäLische Wilhelms-UniversitäT
Design, synthesis, and biological characterization of a caspase 3/7 selective isatin labeled with 2-[18F]fluoroethylazide.
Imperial College
Structure-based discovery of a novel non-peptidic small molecular inhibitor of caspase-3.
Tokyo University of Science
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids.
Epicept
Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors.
Washington University
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.
Merck Frosst Centre For Therapeutic Research
Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo.
University of Edinburgh
5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis.
University Hospital of The WestfäLische Wilhelms-UniversitäT
Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors.
Procter & Gamble Pharmaceuticals
Synthesis and Biological Evaluation of Celastrol Derivatives with Improved Cytotoxic Selectivity and Antitumor Activities.
China Pharmaceutical University
Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.
Washington University
Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.
Procter & Gamble Pharmaceuticals
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Shandong University
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.
Procter & Gamble Pharmaceuticals
Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents.
Maxim Pharmaceuticals
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme.
Procter & Gamble Pharmaceuticals
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.
Maxim Pharmaceuticals
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
Shandong University
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Merck Frosst Centre For Therapeutic Research
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
University of Illinois At Chicago
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.
Maxim Pharmaceuticals
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Idun Pharmaceuticals
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Galapagos
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Idun Pharmaceuticals
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.
Idun Pharmaceuticals
Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.
Idun Pharmaceuticals
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.
Merck Research Laboratories
Quinolone hybrids and their anti-cancer activities: An overview.
Qilu University of Technology (Shandong Academy of Sciences)
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Roche Pharma Research and Early Development
Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.
Basf Bioresearch
Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines.
Hebei University of Science & Technology
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).
Idun Pharmaceuticals
Development of a potent and selective cell penetrant Legumain inhibitor.
Queen'S University Belfast
Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.
Harbor Branch Oceanographic Institution
Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella.
Harbor Branch Oceanographic Institution
Structure-activity relationship study of a series of caspase inhibitors containing γ-amino acid moiety for treatment of cholestatic liver disease.
Wuxi Apptec (Shanghai)
Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.
Nestl�
Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.
Progenra
Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.
Emory Chemical Biology Discovery Center Emory University School of Medicine Atlanta
Imidazopyrazine compounds, preparation methods and uses thereof
Dongguan Zhenxing-Beite Medicine Technology
Pyrazolopyrimidine compounds for the treatment of cancer
University of North Carolina At Chapel Hill
Evolution of Src Homology 2 (SH2) Domain to Recognize Sulfotyrosine.
University of Nebraska-Lincoln
Heterocyclic sulfone mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
N-[9-(ortho-fluorobenzyl)-2-phenyl-8-azapurin-6-yl]-amides as potent and selective ligands for A1 adenosine receptors.
University of Pisa
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Wyeth Research
Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
Guilford Pharmaceuticals
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Merck Research Laboratories
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.
Astrazeneca
Novel Indolocarbazole protein kinase C inhibitors with improved biochemical and physicochemical properties.
Tumor Biology Center
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).
Dupont Pharmaceuticals
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.
Medivir