Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: Derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge |
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| Authors: | Nancy Ty Julia Kaffy Alban Arrault Sylviane Thoret Renée Pontikis Joelle Dubois Luc Morin-Allory Jean-Claude Florent |
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| Affiliation: | 1. Institut Curie, Centre de Recherche, 26 rue d’Ulm, 75248 Paris, France;2. CNRS, UMR 176, 26 rue d’Ulm, 75248 Paris, France;3. ICOA, Université d’Orléans, BP 6759, 45067 Orléans Cedex 2, France;4. CNRS, UMR 6005, 45067 Orléans Cedex 2, France;5. ICSN, CNRS, UPR 2301, Avenue de la Terrasse, 91198 Gif-sur-Yvette, France |
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| 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. |
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