Issue 22, 2011
From the journal:

Organic & Biomolecular Chemistry

Synthesis and biological activity of optimized belactosin C congeners†

Vadim S. Korotkov,a   Antje Ludwig,b   Oleg V. Larionov,a   Alexander V. Lygin,a   Michael Grollc  and  Armin de Meijere*a  

* Corresponding authors

a Institut für Organische und Biomolekulare Chemie der Georg-August-Universität Göttingen, Tammannstrasse 2, Germany
E-mail: Armin.deMeijere@chemie.uni-goettingen.de

b Charité Universitätsmedizin Berlin CCM Med. Klinik für Kardiologie und Angiologie Kardiologisches Forschungslabor Ziegelstrasse 5-9, Germany

c Center for Integrated Protein Science at the Department Chemie, Lehrstuhl für Biochemie, Technische Universität München, Garching, Germany

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.

Graphical abstract: Synthesis and biological activity of optimized belactosin C congeners

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Article information

DOI
https://doi.org/10.1039/C1OB05661A
Article type
Paper
Submitted
27 Apr 2011
Accepted
11 Aug 2011
First published
23 Sep 2011

Org. Biomol. Chem., 2011,9, 7791-7798

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Synthesis and biological activity of optimized belactosin C congeners

V. S. Korotkov, A. Ludwig, O. V. Larionov, A. V. Lygin, M. Groll and A. de Meijere, Org. Biomol. Chem., 2011, 9, 7791 DOI: 10.1039/C1OB05661A

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