From meiogynin A to the synthesis of dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins

The synthesis of one of the most potent dual inhibitors of the anti-apoptotic proteins Bcl-xL and Mcl-1 is reported. This analogue of a natural sesquiterpenoid dimer meiogynin A was elaborated by a convergent asymmetric synthesis with 36% yield in ten steps.

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2014-08, Vol.50 (62), p.8593-8596
Main Authors: Desrat, S, Remeur, C, Gény, C, Rivière, G, Colas, C, Dumontet, V, Birlirakis, N, Iorga, B I, Roussi, F
Format: Article
Language:English
Subjects:
Analogue
Asymmetry
bcl-X Protein - antagonists & inhibitors
bcl-X Protein - metabolism
Chemical Sciences
Cycloaddition Reaction - methods
Dimers
Inhibitors
Models, Molecular
Molecular Docking Simulation
Myeloid Cell Leukemia Sequence 1 Protein - antagonists & inhibitors
Myeloid Cell Leukemia Sequence 1 Protein - metabolism
Organic chemistry
Proteins
Sesquiterpenes - chemical synthesis
Sesquiterpenes - pharmacology
Synthesis
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Description
Summary:The synthesis of one of the most potent dual inhibitors of the anti-apoptotic proteins Bcl-xL and Mcl-1 is reported. This analogue of a natural sesquiterpenoid dimer meiogynin A was elaborated by a convergent asymmetric synthesis with 36% yield in ten steps.
ISSN:1359-7345
1364-548X
DOI:10.1039/c4cc01830c