Synthesis and biological activity of optimized belactosin C congeners

Vadim S. Korotkov; Antje Ludwig; Oleg V. Larionov; Alexander V. Lygin; Michael Groll; Armin De Meijere

doi:10.1039/c1ob05661a

Synthesis and biological activity of optimized belactosin C congeners

Vadim S. Korotkov, Antje Ludwig, Oleg V. Larionov, Alexander V. Lygin, Michael Groll, Armin De Meijere

Chair of Biochemistry

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22 Scopus citations

Abstract

Successful biochemical studies of the natural products belactosin A and C as well as their more stable acylated derivatives have proved them to be powerful proteasome inhibitors and thereby potential candidates as pharmacologically relevant active compounds. In order to understand their structure-biological activity relations in detail and to find ways of improving their biological activity, four new modified belactosin congeners have been synthesized and tested. One of them (compound 6) turned out to be a more potent inhibitor against HeLa cells than the known proteasome inhibitor MG132.

Original language	English
Pages (from-to)	7791-7798
Number of pages	8
Journal	Organic and Biomolecular Chemistry
Volume	9
Issue number	22
DOIs	https://doi.org/10.1039/c1ob05661a
State	Published - 26 Oct 2011

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AU - Ludwig, Antje

AU - Larionov, Oleg V.

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AU - Groll, Michael

AU - De Meijere, Armin

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Synthesis and biological activity of optimized belactosin C congeners

Abstract

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