Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 7, Pages 2157-2160Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm900047j
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- DFG (Deutsche Forschungsgemeinschaft)
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This paper describes the synthesis and biological evaluation of a new class of peptidomimetic falcipain-2 inhibitors based on a 1,4-benzodiazepine scaffold combined with various alpha,beta-unsaturated electrophilic functions such as vinyl-ketone, -amide, -ester, and -nitrile. The profile of reactivity of this class of derivatives has been evaluated and 4c, containing a vinyl ester warhead, proved to be a highly potent and selective falcipain-2 inhibitor.
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