Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid

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 P2 amino acid. The SAR studies also showed that the Asp free carboxylic acid in P1 is important for caspase inhibiting activities, as well as for selectivity over other proteases. [Copyright &y& Elsevier]