Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6

Wenhua Chu, Justin Rothfuss, Yunxiang Chu, Dong Zhou, Robert H. Mach

Research output: Contribution to journalArticlepeer-review

43 Scopus citations

Abstract

A key step in the onset of Huntington's disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments. Therefore, the inhibition of caspase-6 has been identified as a target for therapeutic drug development for the treatment of this disease. In this study, a series of isatin sulfonamide Michael acceptors having a high nanomolar potency for inhibiting caspase-6 and increased selectivity for caspase-6 versus caspase-3 inhibition is reported.

Original languageEnglish
Pages (from-to)2188-2191
Number of pages4
JournalJournal of Medicinal Chemistry
Volume52
Issue number8
DOIs
StatePublished - Apr 23 2009

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