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Synthesis and biological evaluation of new bis-indolone-N-oxides. | LitMetric

Synthesis and biological evaluation of new bis-indolone-N-oxides.

Bioorg Chem

Université de Toulouse III, UPS, UMR 152 PHARMA-DEV, 118 Route de Narbonne, F-31062 Toulouse cedex 9, France.

Published: June 2013

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.

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http://dx.doi.org/10.1016/j.bioorg.2013.03.001DOI Listing

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