Horizon 1 1 17 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES Synthesis and antiplasmodial activity of new indolone N-oxide derivatives Journal of Medicinal Chemistry 699-714 2010 PAR00004660 ENG Journal of Medicinal Chemistry 0022-2623 ISI:000273672100017 2 10.1021/jm901300d https://www.documentation.ird.fr/hor/PAR00004660 53 Horizon (IRD) 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. 020 ; 052 UR152 Cameroun