Abstract
Various heterocyclic hetero-methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A study of their structure-activity relationship (SAR) related to caspase-1, -3, -6, and -8 is reported. Their efficacy in a cellular model of cell death is also discussed. Potent broad-spectrum caspase inhibitors have been identified.
MeSH terms
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Animals
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Aspartic Acid / chemistry
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Caspase Inhibitors*
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Cell Death / drug effects*
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Cells, Cultured
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Cysteine Proteinase Inhibitors / pharmacology*
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / pharmacology*
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Ketones / chemical synthesis
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Ketones / pharmacology*
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Mice
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Models, Biological
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Naphthols / chemistry
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Structure-Activity Relationship
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Valine / chemistry
Substances
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Caspase Inhibitors
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Cysteine Proteinase Inhibitors
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Heterocyclic Compounds
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Ketones
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Naphthols
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naphthyl acetate
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Aspartic Acid
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Valine