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J Med Chem ; 53(2): 699-714, 2010 Jan 28.
Article in English | MEDLINE | ID: mdl-20014857

ABSTRACT

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.), as well as for cytotoxic concentration (CC(50)) 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 (CC(50) MCF7/IC(50) FcB1: 14623; CC(50) KB/IC(50) 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.


Subject(s)
Antimalarials/chemical synthesis , Indoles/chemical synthesis , Animals , Antimalarials/pharmacology , Cell Line, Tumor , Drug Resistance , Humans , Indoles/pharmacology , Oxides/chemical synthesis , Oxides/pharmacology , Parasitemia/drug therapy , Parasitic Sensitivity Tests , Plasmodium berghei/drug effects , Plasmodium falciparum/drug effects , Structure-Activity Relationship
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