Nepveu Françoise auteur aut IRD Kim S. auteur aut IRD Boyer J. auteur aut IRD Chatriant O. auteur aut IRD Ibrahim H. auteur aut IRD Reybier K. auteur aut IRD Monje M. C. auteur aut IRD Chevalley Sèverine auteur aut IRD Perio P. auteur aut IRD Lajoie B. H. auteur aut IRD Bouajila J. auteur aut IRD Deharo Eric auteur aut IRD Sauvain Michel auteur aut IRD Tahar Rachida auteur aut IRD Basco Leonardo auteur aut IRD Pantaleo A. auteur aut IRD Turini F. auteur aut IRD Arese P. auteur aut IRD Valentin A. auteur aut IRD Thompson E. auteur aut IRD Vivas L. auteur aut IRD Petit S. auteur aut IRD Nallet J. P. auteur aut IRD text journalArticle eng A series of 66 new indolone-N-oxide derivatives was synthesized with three different methods. Compounds were evaluated for in vitro activity against CQ-sensitive (3D7), CQ-resistant (FcB1), and CQ and pyrimethamine cross-resistant (K1) strains of Plasmodium falciparum (P.f.), its well as for cytotoxic concentration (CC50) on MCF7 and KB human tumor Cell lines. Compound 26 (5-methoxy-indolone-N-oxide analogue) had the most potent antiplasmodial activity in vitro (< 3 nM on FcB1 and = 1.7 nM on 3D7) with a very satisfactory selectivity index (CC50 MCF7/IC50 FcB1: 14623; CC50 KB/IC50 3D7: 198823). In in vivo experiments, compound 1 (dioxymethylene derivatives of the indolone-N-oxide) showed the best antiplasmodial activity against Plasmodium berghei, 62% inhibition of the parasitaemia at 30 mg/kg/day. specialized 020 052 53 2 699-714 2010 0022-2623 https://www.documentation.ird.fr/hor/PAR00004660 10.1021/jm901300d 0022-2623 https://www.documentation.ird.fr/hor/PAR00004660 IRD - Base Horizon / Pleins textes 2010-03-10 2017-08-23 PAR00004660 fre