Isatin sulfonamide analogs containing a Michael addition acceptor: A new class of caspase 3/7 inhibitors

Wenhua Chu, Justin Rothfuss, André D'Avignon, Chenbo Zeng, Dong Zhou, Richard S. Hotchkiss, Robert H. Mach

Research output: Contribution to journalArticlepeer-review

75 Scopus citations

Abstract

A series of isatin sulfonamide analogs having a Michael acceptor were prepared and their potencies for inhibiting caspase-1, -3, -6, -7, and -8 were evaluated. These compounds have nanomolar potency for inhibiting the executioner caspases, caspase-3 and caspase-7, and have a low potency for inhibiting caspase-1, caspase-6, and caspase-8. The inhibition mechanism was investigated through NMR studies of the reaction between 11d and benzylmercaptan as a model for Cys-285 in the active site of caspase-3.

Original languageEnglish
Pages (from-to)3751-3755
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
Issue number15
DOIs
StatePublished - Jul 26 2007

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