PMID

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Article Title

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Variation of the aryl substituent on the piperazine ring within the 4-(piperazin-1-yl)-2,6-di(pyrrolidin-1-yl)pyrimidine scaffold unveils potent, non-competitive inhibitors of the inflammatory caspases.

Depaul University

Inhibiting the Inflammasome: A Chemical Perspective.

The University of Manchester

Azaphilones from an Acid Mine Extremophile Strain of a Pleurostomophora sp.

Memorial Sloan-Kettering Cancer Center

Electrophilic warhead-based design of compounds preventing NLRP3 inflammasome-dependent pyroptosis.

University of Turin

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

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

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

Protease inhibitors: current status and future prospects.

University of Queensland

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

Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.

Washington University

Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones.

Pfizer

Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).

Pfizer

Noncovalent tripeptidyl benzyl- and cyclohexyl-amine inhibitors of the cysteine protease caspase-1.

The University of Queensland

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

National Human Genome Research Institute

 

3-chloro-4-carboxamido-6-arylpyridazines as a non-peptide class of interleukin-1β converting enzyme inhibitor

TBA

 

Structure-based design of non-peptidic pyridone aldehydes as inhibitors of interleukin-1β converting enzyme

TBA

 

PYRIDONE-BASED PEPTIDOMIMETIC INHIBITORS OF INTERLEUKIN-1β-CONVERTING ENZYME (ICE)

TBA

 

Structural and stereochemical requirements of time-dependent inactivators of the interleukin-1β converting enzyme

TBA

 

Inhibition of interleukin-1β converting enzyme by N-acyl-aspartyl aryloxymethyl ketones

TBA

 

Inhibition of interleukin-1β converting enzyme by N-Acyl-aspartic acid ketones

TBA

 

The synthesis and evaluation of peptidyl aspartyl aldehydes as inhibitors of ice.

TBA

 

Activated ketones as potent reversible inhibitors of interleukin-Iβ converting enzyme

TBA

 

Synthesis of a peptidyl 2,2-difluoro-4-phenylbutyl ketone and its evaluation as an inhibitor of interleukin-1β converting enzyme.

TBA

 

Phenylalkyl ketones as potent reversible inhibitors of interleukin-1β converting enzyme

TBA

 

Synthesis of a potent, reversible inhibitor of interleukin-1β converting enzyme

TBA

Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis.

Westfalische Wilhelms-Universitat

Design, synthesis, and biological characterization of a caspase 3/7 selective isatin labeled with 2-[18F]fluoroethylazide.

Imperial College

Recent developments in fragment-based drug discovery.

Astex Therapeutics

The berkeleyamides, amides from the acid lake fungus Penicillum rubrum.

Montana Tech of The University of Montana

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

Furazans in Medicinal Chemistry.

Treventis

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

Design, synthesis and biological evaluation of 1,5-disubstituted ?-amino tetrazole derivatives as non-covalent inflammasome-caspase-1 complex inhibitors with potential application against immune and inflammatory disorders.

National Research Council (Cnr)

Tethering identifies fragment that yields potent inhibitors of human caspase-1.

Sunesis Pharmaceuticals

Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.

Procter & Gamble Pharmaceuticals

Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme.

Procter & Gamble Pharmaceuticals

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

Merck Frosst Centre For Therapeutic Research

Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.

Pfizer

Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1? Axis.

University of Rhode Island

The design and synthesis of sulfonamides as caspase-1 inhibitors.

Pfizer

Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.

Senju Pharmaceutical

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

A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors.

Vertex Pharmaceuticals

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

Basf Bioresearch

Rapid optimization of an ICE inhibitor synthesis using multiple reaction conditions in a parallel array.

Warner-Lambert

Novel cytokine release inhibitors. Part I: Triterpenes.

RhóNe-Poulenc Rorer Central Research

Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).

Ferring Research Institute

Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1 beta-converting enzyme inhibitor.

Sanofi Winthrop

New Caspase-1 inhibitor by scaffold hopping into bio-inspired 3D-fragment space.

Edelris

Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.

Nestl�

(S)-3-(2-(4-(benzyl)-3-oxopiperazin-1-yl)acetamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid derivatives and related compounds as caspase inhibitors for treating cardiovascular diseases

Histogen

Selective caspase inhibitors and uses thereof

Genesis Technologies

Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors.

University of Colorado

Lazaroids U83836E and U74389G are potent, time-dependent inhibitors of caspase-1.

Depaul University

Selective caspase inhibitors and uses thereof

Novagenesis Foundation

Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.

Washington University

Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide.

Pfizer

Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1).

Pfizer

Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.

Merck Frosst Canada

Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors.

Merck Frosst Canada

N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies.

Washington University

Potent and selective nonpeptide inhibitors of caspases 3 and 7.

Glaxosmithkline

Inhibition of human caspases by peptide-based and macromolecular inhibitors.

Merck Research Laboratories

Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.

Sunesis Pharmaceuticals