918542-07-1Relevant articles and documents
NOVEL STEROIDS AND METHODS OF MANUFACTURE
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Page/Page column 87, (2019/03/05)
The present disclosure relates to methods of producing enantiodefined polycyclic ring compounds. More particularly, the present disclosure provides synthetic methods of producing biologically active enantiodefined steroidal compositions of both natural and unnatural ("ent-") absolute stereochemistry. The present disclosure also relates to methods of using said steroidal compositions prepared from this method as biologically active (e.g., therapeutic) components in compositions and/or directly as human and/or animal therapeutics and medicines. The present disclosure further relates to methods of producing and using said steroidal compositions of matter in chemical, pharmacological, and biological studies and research.
Synthesis and antiplasmodial activity of new indolone N-Oxide derivatives
Nepveu, Fran?oise,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
experimental part, p. 699 - 714 (2010/07/09)
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 (P.f.), aswell 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 antiplasmodial activity in vitro (50 MCF7/IC50 FcB1: 14623; CC50 KB/IC50 3D7: 198823). In in vivo experiments, compound 1 (dioxymethylene derivatives of the indolone-N-oxide) showed the best antiplasmodial activity against Plasmodium berghei, 62% inhibition of the parasitaemia at 30 mg/kg/day. 2009 American Chemical Society.