Synthesis and Evaluation of Antiplasmodial Activities of Fluorinated 6-Amino- 2-Aryl-3H-Indolone-N-Oxides
Journal Title: UNKNOWN - Year 2018, Vol 8, Issue 4
Abstract
A series of novel 6-amino-2-aryl-3H-indolone-N-oxides were synthesized at yields of up to 65% and characterized; one was further characterized using X-ray crystallographic analysis. Synthesized compounds were evaluated for their in vitro activity against a chloroquine-resistant (FcB1) strain of Plasmodium falciparum, as well as for the 50% cytotoxic concentration (CC50) on Vero cell lines. The most promising activities were observed for the fluorinated compounds, the most active in vitro being 6-(2-morpholinoacetamido)-2-(4-(trifluoromethoxy) phenyl)-3H-indolone-N-oxide (IC50: 15.5 nM). In addition, these compounds showed weak cytotoxicity leading to selectivity index values of >170, thus warranting further in vitro and in vivo studies.
Authors and Affiliations
Amani Mejai, Ennaji Najahi, Gneigny Tchan, Pierre Perio, Laure Vendier, Sandra Bourgeade Delmas, Rym Abidi, Mohamed Haddad, Françoise Nepveu, Karine Reybie
Keywords
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