Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group

…, S Jia, Y Wang, W Yang, B Tseng, J Drewe

Index: Cai, Sui Xiong; Guan, Lufeng; Jia, Shaojuan; Wang, Yan; Yang, Wu; Tseng, Ben; Drewe, John Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 21 p. 5295 - 5300

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Citation Number: 25

Abstract

This article describes the synthesis and biological evaluation of a group of N-protected Val- Asp-fmk as caspase inhibitors. The protecting group was found to contribute to caspase-3 inhibiting activity, and compounds with a large group such as Cbz are more active than compounds with a small group such as Ac. Compounds with more hydrophobic protecting groups were found to be more active in cell apoptosis protection assays, probably due to ...