Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
作者信息
Wang Yan, Huang Jin-Chen, Zhou Zhang-Lin, Yang Wu, Guastella John, Drewe John, Cai Sui Xiong
机构信息
Maxim Pharmaceuticals, 6650 Nancy Ridge Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1269-72. doi: 10.1016/j.bmcl.2003.12.065.
PMID:14980679
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.
摘要
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