2. Academic Validation
  3. Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues

Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues

  • Eur J Med Chem. 2011 Jan;46(1):95-100. doi: 10.1016/j.ejmech.2010.10.018.
Martin Arthuis 1,  Renée Pontikis,  Guy G Chabot,  Lionel Quentin,  Daniel Scherman,  Jean-Claude Florent
Affiliations

Affiliation

  • 1 Institut Curie, Centre de Recherche, 26 rue d'Ulm, Paris F-75248 cedex 05, France.
PMID: 21112130 DOI: 10.1016/j.ejmech.2010.10.018
Abstract

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.

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