Peptidyl allyl sulfones: a new class of inhibitors for clan CA cysteine proteases

MG Götz, CR Caffrey, E Hansell, JH McKerrow…

Index: Goetz, Marion G.; Caffrey, Conor R.; Hansell, Elizabeth; McKerrow, James H.; Powers, James C. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 19 p. 5203 - 5211

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Citation Number: 37

Abstract

A new series of peptidyl allyl sulfone inhibitors was discovered while trying to synthesize epoxy sulfone inhibitors from vinyl sulfones using basic oxidizing conditions. The various dipeptidyl allyl sulfones were evaluated with calpain I, papain, cathepsins B and L, cruzain and rhodesain and found to be potent inhibitors. In comparison to the previously developed class of vinyl sulfone inhibitors, the novel dipeptidyl allyl sulfones were more potent ...