Abstract
Caspase-3 is a cysteinyl protease that mediates apoptotic cell death. Its inhibition may have an important impact on the treatment of several degenerative diseases. Here we report the synthesis of reversible inhibitors via a solid-support palladium-catalyzed amination of 3-bromopyrazinones and the discovery of a pan-caspase reversible inhibitor.
MeSH terms
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Amination
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Caspase Inhibitors*
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Catalysis
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Cell Line
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Chromatography, High Pressure Liquid
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Humans
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Indicators and Reagents
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Mass Spectrometry
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Palladium / chemistry*
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology*
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Pyrazines / chemical synthesis*
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Pyrazines / pharmacology*
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Recombinant Proteins / chemistry
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Structure-Activity Relationship
Substances
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Caspase Inhibitors
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Indicators and Reagents
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Protease Inhibitors
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Pyrazines
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Recombinant Proteins
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Palladium