1. Synthesis and biological evaluation of new bis-indolone-N-oxides.
- Author
-
Najahi E, Valentin A, Téné N, Treilhou M, and Nepveu F
- Subjects
- Anti-Infective Agents pharmacology, Anti-Infective Agents toxicity, Antimalarials pharmacology, Antimalarials toxicity, Bacteria drug effects, Candida drug effects, Cell Survival drug effects, Humans, MCF-7 Cells, Microbial Sensitivity Tests, Oxides chemical synthesis, Oxides pharmacology, Plasmodium falciparum drug effects, Anti-Infective Agents chemical synthesis, Antimalarials chemical synthesis, Indoles chemistry, Oxides chemistry
- 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., (Copyright © 2013 Elsevier Inc. All rights reserved.)
- Published
- 2013
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