title: Synthesis and biological evaluation of new bis-indolone-N-oxides.
abstract: A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They did not cause any haemolysis (300 μgmL(-1)). Of the synthesized bis-indolones, compound 1a had the most potent antiplasmodial activity (IC50=0.763 μmolL(-1) on the FcB1 strain) with a selectivity index (CC50 MCF7/IC50 FcB1) of 35.6. No potency against the tested microbial strains was observed.
authors: Université de Toulouse III, UPS, UMR 152 PHARMA-DEV, 118 Route de Narbonne, F-31062 Toulouse cedex 9, France. ennaji.najahi@univ-tlse3.fr
authors: Ennaji
authors: E
authors: Najahi
authors: Alexis
authors: A
authors: Valentin
authors: Nathan
authors: N
authors: Téné
authors: Michel
authors: M
authors: Treilhou
authors: Françoise
authors: F
authors: Nepveu
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001419:Bacteria / Q000187:drug effects; D002175:Candida / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D061986:MCF-7 Cells; D008826:Microbial Sensitivity Tests; D010087:Oxides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects
chemical_list: D000890:Anti-Infective Agents; D000962:Antimalarials; D007211:Indoles; D010087:Oxides; C030374:indole