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ID: ALA1144434

Journal: Bioorg Med Chem Lett

Title: Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads.

Authors: Ullman BR, Aja T, Chen N, Diaz JL, Gu X, Herrmann J, Kalish VJ, Karanewsky DS, Kodandapani L, Krebs JJ, Linton SD, Meduna SP, Nalley K, Robinson ED, Roggo SP, Sayers RO, Schmitz A, Ternansky RJ, Tomaselli KJ, Wu JC.

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.

CiteXplore: 15964758

DOI: 10.1016/j.bmcl.2005.05.036