1. Academic Validation
  2. Synthesis and antiprotozoal activity of 4-arylcoumarins

Synthesis and antiprotozoal activity of 4-arylcoumarins

  • Eur J Med Chem. 2010 Mar;45(3):864-9. doi: 10.1016/j.ejmech.2009.10.022.
Jean-Thomas Pierson 1 Aurélien Dumètre Sébastien Hutter Florence Delmas Michèle Laget Jean-Pierre Finet Nadine Azas Sébastien Combes
Affiliations

Affiliation

  • 1 Faculté des Sciences de Saint-Jérôme, UMR-CNRS 6264, Laboratoire Chimie Provence, Universités Aix-Marseille I, II and III, 13397 Marseille Cedex 20, France.
Abstract

A large series of 4-arylcoumarins was synthesized by Suzuki-Miyaura cross-coupling reaction and evaluated for antiprotozoal activity against Plasmodium falciparum and Leishmania donovani. Several compounds were found to strongly inhibit the proliferation of human cell line and/or parasites. The 4-(3,4-dimethoxyphenyl)-6,7-dimethoxycoumarin exhibit a potent activity on L. donovani amastigotes with a selectivity index (SI=265) twice than amphotericin B (SI=140).

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