PMID

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Article Title

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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

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

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

Irreversible inhibitors of cysteine proteases.

Dart Neuroscience

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University of Florida

Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.

Maxim Pharmaceuticals

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

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, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.

Washington University

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.

Maxim Pharmaceuticals

Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.

Merck Frosst Centre For Therapeutic Research

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.

Maxim 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

Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.

Basf Bioresearch

In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.

Merck Research Laboratories

Molecular cloning and characterization of a new receptor for galanin.

Merck Research Laboratories

The molecular interactions of buspirone analogues with the serotonin transporter.

National Medicines Institute

Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.

National Taiwan University

Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.

Irbm/Merck Research Laboratories

Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.

Targegen

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Piramed Pharma

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

Bristol-Myers Squibb