Potent and selective nonpeptide inhibitors of caspases 3 and 7

D Lee, SA Long, JH Murray, JL Adams…

Index: Lee; Long; Murray; Adams; Nuttall; Nadeau; Kikly; Winkler; Sung; Ryan; Levy; Keller; DeWolf Jr. Journal of Medicinal Chemistry, 2001 , vol. 44, # 12 p. 2015 - 2026

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Citation Number: 166

Abstract

5-Dialkylaminosulfonylisatins have been identified as potent, nonpeptide inhibitors of caspases 3 and 7. The most active compound within this series (34) inhibited caspases 3 and 7 in the 2-6 nM range and exhibited approximately 1000-fold selectivity for caspases 3 and 7 versus a panel of five other caspases (1, 2, 4, 6, and 8) and was at least 20-fold more selective versus caspase 9. Sequence alignments of the active site residues of the ...