title: In vitro activities of new 2-substituted quinolines against Leishmania donovani.
abstract: A series of 9 quinolines and 18 styrylquinolines was evaluated for the drugs' in vitro antileishmanial activities and cytotoxicities. The 7-aroylstyrylquinoline scaffold appeared to be the most promising one, with the most interesting compound, no. 35, exhibiting a 50% inhibitory concentration (IC(50)) of 1.2 μM and a selectivity index value of 121.5. Compound 35 was 10-fold and 8-fold more active than miltefosine and sitamaquine, the reference compounds, with selectivity indexes 607-fold and 60-fold higher, respectively.
authors.affiliation: Groupe Chimiothérapie Antiparasitaire, UMR 8076 CNRS BioCis, Faculté de Pharmacie, Université Paris-Sud, 92290-Châtenay-Malabry, France. philippe.loiseau@u-psud.fr
authors.forename: Philippe M
authors.initials: PM
authors.lastname: Loiseau
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
authors.forename: Aditya
authors.initials: A
authors.lastname: Verma
authors.forename: Saumya
authors.initials: S
authors.lastname: Srivastava
authors.forename: S K
authors.initials: SK
authors.lastname: Puri
authors.forename: Faten
authors.initials: F
authors.lastname: Sliman
authors.forename: Marie
authors.initials: M
authors.lastname: Normand-Bayle
authors.forename: Didier
authors.initials: D
authors.lastname: Desmaele
mesh_terms: D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D015394:Molecular Structure; D011804:Quinolines / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000494:pharmacology*
chemical_list: D011804:Quinolines; D014344:Trypanocidal Agents