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ID: ALA1147604
Journal: Bioorg Med Chem Lett
Title: Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Authors: Wang Y, Huang JC, Zhou ZL, Yang W, Guastella J, Drewe J, Cai SX.
Abstract: This article describes the synthesis and biological evaluation of a series of dipeptidyl aspartyl fluoromethylketones as caspase-3 inhibitors. Structure-activity relationship (SAR) studies showed that for caspase-3 inhibition, Val is the best P(2) amino acid. The SAR studies also showed that the Asp free carboxylic acid in P(1) is important for caspase inhibiting activities, as well as for selectivity over other proteases.
CiteXplore: 14980679