Issue 31, 2012

Synthesis and biological activity of simplified belactosin C analogues

Abstract

Successful biochemical studies of the natural products belactosin A and C and their acylated congeners have shown a β-lactonecarboxamide moiety to be a possible core structure of powerful proteasome inhibitors. As a part of further investigations, variously decorated simplified β-lactonecarboxamides have been synthesized in order to understand structure–biological activity relations in detail, to find ways of improving their biological activity and stability and to reduce the complexity of their preparation. Biological tests showed that the best compounds possess a high potential against phytopathogenic fungi in the greenhouse.

Graphical abstract: Synthesis and biological activity of simplified belactosin C analogues

Supplementary files

Article information

Article type
Paper
Submitted
19 Mar 2012
Accepted
13 Jun 2012
First published
26 Jun 2012

Org. Biomol. Chem., 2012,10, 6363-6374

Synthesis and biological activity of simplified belactosin C analogues

A. de Meijere, V. S. Korotkov, A. V. Lygin, O. V. Larionov, V. V. Sokolov, T. Graef and M. Es-Sayed, Org. Biomol. Chem., 2012, 10, 6363 DOI: 10.1039/C2OB25586C

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