Abstract
A series of potent dipeptide and tripeptide alpha-ketohydroxamic esters was prepared as inhibitors of recombinant human calpain I. Compound 3c, a Cbz-Leu-Phe hydroxamate, displayed the greatest potency against calpain I (IC(50)=6nM), while two compounds, 3l and 3m, both possessing the Cbz-Leu-Leu-Phe sequence, were the most potent (IC(50)=0.2 microM) in a MOLT-4 cell assay.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Calpain / antagonists & inhibitors*
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Cell Membrane Permeability / drug effects
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Glycoproteins / chemical synthesis
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Glycoproteins / chemistry
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Glycoproteins / pharmacology*
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Humans
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Ketones / chemical synthesis
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Ketones / chemistry
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Ketones / pharmacology*
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Oligopeptides / chemical synthesis
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Recombinant Proteins / antagonists & inhibitors
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Structure-Activity Relationship
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Tumor Cells, Cultured / drug effects
Substances
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Glycoproteins
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Ketones
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Oligopeptides
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Recombinant Proteins
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calpain inhibitors
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Calpain