期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 1, 页码 95-100出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.10.018
关键词
Combretastatin; Phenstatin; Aroylindole; Tubulin; Cytotoxicity
资金
- Centre National de la Recherche Scientifique (CNRS)
- Institut Curie
- Institut National de la Sante et de la Recherche Medicale (Inserm)
- Institut National du Cancer (INCa, Boulogne Billancourt, France)
- Ministere de l'Enseignement Superieur et de la Recherche
Two series of 2-aroyltrimethoxyindoles were designed to investigate the effects of the replacement of the trimethoxyphenyl ring of phenstatin with a trimethoxyindole moiety. These compounds were efficiently prepared through a domino palladium-catalyzed sequence from 2-gem-dibromovinylanilines substituted by three methoxy groups and arylboronic acids under carbon monoxide atmosphere. These novel heterocyclic combretastatin A4 analogues were evaluated for their cell growth inhibitory properties and their ability to inhibit the tubulin polymerization. (C) 2010 Elsevier Masson SAS. All rights reserved.
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