Discovery of a new antileishmanial hit in 8-nitroquinoline series

…, P Verhaeghe, M Casanova, C Castera-Ducros…

Index: Paloque, Lucie; Verhaeghe, Pierre; Casanova, Magali; Castera-Ducros, Caroline; Dumetre, Aurelien; Mbatchi, Litaty; Hutter, Sebastien; Kraiem-M'Rabet, Manel; Laget, Michele; Remusat, Vincent; Rault, Sylvain; Rathelot, Pascal; Azas, Nadine; Vanelle, Patrice European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 75 - 86

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Citation Number: 25

Abstract

A series of nitrated 2-substituted-quinolines was synthesized and evaluated in vitro toward Leishmania donovani promastigotes. In parallel, the in vitro cytotoxicity of these molecules was assessed on the murine J774 and human HepG2 cell lines. Thus, a very promising antileishmanial hit molecule was identified (compound 21), displaying an IC50 value of 6.6 μM and CC50 values≥ 100 μM, conferring quite good selectivity index to this molecule, in ...