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ID: ALA1136077
Journal: Bioorg Med Chem Lett
Title: Nicotinyl aspartyl ketones as inhibitors of caspase-3.
Authors: Isabel E, Black WC, Bayly CI, Grimm EL, Janes MK, McKay DJ, Nicholson DW, Rasper DM, Renaud J, Roy S, Tam J, Thornberry NA, Vaillancourt JP, Xanthoudakis S, Zamboni R.
Abstract: Caspase-3 is a cysteinyl protease that mediates apoptotic cell death. Its inhibition may have an important impact in the treatment of several degenerative diseases. Since P(1) aspartic acid is a required element of recognition for this enzyme, a library of capped aspartyl aldehydes was synthesized using solid-phase chemistry. The 5-bromonicotinamide derivative of the aspartic acid aldehyde was identified to be an inhibitor of caspase-3. Substitution at the 5-position of the pyridine ring and conversion of the aldehyde to ketones led to a series of potent inhibitors of caspase-3.
CiteXplore: 12798321