Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4 |
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| Authors: | Thi Thanh Binh Nguyen Thierry Lomberget Ngoc Chau Tran Evelyne Colomb Lore Nachtergaele Sylviane Thoret Joëlle Dubois Joren Guillaume Rawad Abdayem Marek Haftek Roland Barret |
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| Institution: | 1. Université de Lyon, Université Lyon 1, Faculté de Pharmacie, ISPB, EA 4446 Biomolécules, Cancer et Chimiorésistances, SFR Santé Lyon-Est CNRS UMS3453 - INSERM US7, 8 avenue Rockefeller, F-69373 Lyon cedex 08, France;2. Université Lyon 1, Faculté de Médecine et de Pharmacie, EA 4169, Fundamental, clinical and therapeutic aspects of the skin barrier, 8 avenue Rockefeller, F-69373 Lyon cedex 08, France;3. Institut de Chimie des Substances Naturelles, UPR 2301, CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette, France |
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| Abstract: | A novel series of combretastatin A-4 heterocyclic analogues was prepared by replacement of the B ring with indole, benzofurane or benzothiophene, attached at the C2 position. These compounds were evaluated for their abilities to inhibit tubulin assembly: derivative cis 3b, having a benzothiophene, showed an activity similar to those of colchicine or deoxypodophyllotoxine. The antiproliferative and antimitotic properties of cis 3b against keratinocyte cancer cell lines were also evaluated and the intracellular organization of microtubules in the cells after treatment with both stereoisomers of 3b was also determined, using confocal microscopy. |
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