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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Bibliographische Detailangaben
Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2014-08, Vol.50 (62), p.8593-8596
Hauptverfasser:	Desrat, S, Remeur, C, Gény, C, Rivière, G, Colas, C, Dumontet, V, Birlirakis, N, Iorga, B I, Roussi, F
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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