Synthesis and antiplasmodial activity of new indolone N-oxide derivatives

…, S Kim, J Boyer, O Chatriant, H Ibrahim…

Index: Nepveu, Francoise; Kim, Sothea; Boyer, Jeremie; Chatriant, Olivier; Ibrahim, Hany; Reybier, Karine; Monje, Marie-Carmen; Chevalley, Severine; Perio, Pierre; Lajoie, Barbora H.; Bouajila, Jalloul; Deharo, Eric; Sauvain, Michel; Tahar, Rachida; Basco, Leonardo; Pantaleo, Antonella; Turini, Francesco; Arese, Paolo; Valentin, Alexis; Thompson, Eloise; Vivas, Livia; Petit, Serge; Nallet, Jean-Pierre Journal of Medicinal Chemistry, 2010 , vol. 53, # 2 p. 699 - 714

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Citation Number: 28

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 (Pf.), as well as for cytotoxic concentration (CC50) on MCF7 and KB human tumor cell lines. Compound 26 (5-methoxy-indolone-N-oxide analogue) had the most potent ...