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ID: ALA1136305
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Authors: Ullman BR, Aja T, Deckwerth TL, Diaz JL, Herrmann J, Kalish VJ, Karanewsky DS, Meduna SP, Nalley K, Robinson ED, Roggo SP, Sayers RO, Schmitz A, Ternansky RJ, Tomaselli KJ, Wu JC.
Abstract: Various aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum caspase inhibitors have been identified. Their efficacy in cellular models of cell death and inflammation are also discussed.
CiteXplore: 14505683