Design and synthesis of novel protease inhibitors. Tripeptide α′,β′-epoxyketones as nanomolar inactivators of the proteasome

Tripeptide α′,β′-epoxyketones were prepared stereospecifically starting from Boc-[S]-phenylalanine. Diastereomer 5b inhibited the chymotrypsin-like activity of porcine endothelial cell derived proteasome at low nanomolar concentrations. Graphic

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Bibliographic Details
Published in:Tetrahedron letters 1996-01, Vol.37 (9), p.1343-1346
Main Authors: Spaltenstein, Andrew, Leban, Johann J., Huang, Jim J., Reinhardt, Kelli R., Humberto Viveros, O., Sigafoos, Jim, Crouch, Ronald
Format: Article
Language:English
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Summary:Tripeptide α′,β′-epoxyketones were prepared stereospecifically starting from Boc-[S]-phenylalanine. Diastereomer 5b inhibited the chymotrypsin-like activity of porcine endothelial cell derived proteasome at low nanomolar concentrations. Graphic
ISSN:0040-4039
1873-3581
DOI:10.1016/0040-4039(96)00018-4