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Issue 19, 2015
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Development of an efficient route toward meiogynin A-inspired dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins

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Abstract

The synthesis, on a large scale, with very good yield and er via an efficient strategy, of a chiral 4-substituted 2-cyclohexenone intermediate, was a milestone in the synthesis of seven analogues of meiogynin A, a natural sesquiterpenoid dimer. These compounds were elaborated in ten linear steps. Their binding affinities for Bcl-xL and Mcl-1, two proteins of the Bcl-2 family, overexpressed in various types of cancers, were evaluated. This enabled to further SAR studies en route to the elaboration of potent dual inhibitors of anti-apoptotic proteins of the Bcl-2 family.

Graphical abstract: Development of an efficient route toward meiogynin A-inspired dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins

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Article information


Submitted
20 Feb 2015
Accepted
07 Apr 2015
First published
07 Apr 2015

Org. Biomol. Chem., 2015,13, 5520-5531
Article type
Paper
Author version available

Development of an efficient route toward meiogynin A-inspired dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins

S. Desrat, C. Remeur and F. Roussi, Org. Biomol. Chem., 2015, 13, 5520
DOI: 10.1039/C5OB00354G

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