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J Med Chem. 2009 Apr 23;52(8):2188-91. doi: 10.1021/jm900135r.

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

Author information

1
Department of Radiology, Washington University School of Medicine, 510 S. Kingshighway Boulevard, St. Louis, Missouri 63110, USA.

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.

PMID:
19326941
DOI:
10.1021/jm900135r
[Indexed for MEDLINE]

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