期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 78, 期 -, 页码 269-274出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.059
关键词
2-Aryl-3H-indol-3-ones; Deoxygenation; Indolone-N-oxides; Antiplasmodial activity; Electrochemical behaviour
资金
- French National Research Agency [ANR-10-BLAN-0726]
- Agence Nationale de la Recherche (ANR) [ANR-10-BLAN-0726] Funding Source: Agence Nationale de la Recherche (ANR)
The synthesis of indolone derivatives and their antiplasmodial activity in vitro against Plasmodium falciparum at the blood stage are described. The 2-aryl-3H-indol-3-ones were synthesized via deoxygenation of indolone-N-oxides. Electrochemical behaviour, antiplasmodial activity and cytotoxicity on human tumor cell lines were compared to those of indolone-N-oxides. The antiplasmodial IC50 (concentrations at 50% inhibition) of these compounds ranged between 49 and 1327 nM. Among them, the 2(4-dimethylaminophenyl)-5-methoxy-indol-3-one, 7, had the best antiplasmodial activity in vitro (IC50 = 49 nM; FcB1 strain) and selectivity index (SI (CC50 MCF7/IC50 FcB1) = 423.4). Thus, the hits identified in this deoxygenated series correspond to their structural homologs in the N-oxide series with comparable electrochemical behaviour at the nitrogen-carbon double bond. (C) 2014 Elsevier Masson SAS. All rights reserved.
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