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Issue 31, 2012
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Synthesis and biological activity of simplified belactosin C analogues

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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

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Publication details

The article was received on 19 Mar 2012, accepted on 13 Jun 2012 and first published on 26 Jun 2012


Article type: Paper
DOI: 10.1039/C2OB25586C
Org. Biomol. Chem., 2012,10, 6363-6374

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    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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