Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375547 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of novel combretastatin A4 analogues, in which the cis-olefinic bridge is replaced by a cyclopropyl-vinyl or a cyclopropyl-amide moiety, were synthesized and evaluated for inhibition of tubulin polymerization and antiproliferative activity. The derivative 9a with a (cis,E)-cyclopropyl-vinyl unit is the most promising compound. As expected, molecular docking of 9a has shown that only one of the cis-cyclopropyl enantiomers is a good ligand for tubulin.
Graphical abstractDocking of two representative compounds in the colchicine binding site of tubulin is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nancy Ty, Julia Kaffy, Alban Arrault, Sylviane Thoret, Renée Pontikis, Joelle Dubois, Luc Morin-Allory, Jean-Claude Florent,