title: Synthesis and in vitro antiplasmodial activity of ferrocenyl aminoquinoline derivatives.
abstract: The aim of this study was to synthesize a series of ferrocenyl 4-aminoquinolines and to evaluate their activities against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquino-resistant). Some of the ferrocenyl compounds exhibited in vitro antiplasmodial activity in the nM range. In particular, (1R,4R)-N1-(7-chloroquinolin-4-yl)-N4-(ferrocenylmethyl)-N4-methylcyclohexane-1,4-diamine 17 presented the lowest IC50 value (26 nM) against CQ-resistant strains.
authors.affiliation: Université Lille Nord de France, Université de Lille 1, Unité de Catalyse et de Chimie du Solide, UMR CNRS 8181, ENSCL, B.P. 108, 59652 Villeneuve d'Ascq, France; Université des Sciences et Techniques de Masuku, BP 901 Franceville, Gabon.
authors.forename: Gabin
authors.initials: G
authors.lastname: Mwande Maguene
authors.affiliation: Centre International de Recherches Médicales de Franceville (CIRMF), Unité de Parasitologie, BP 769 Franceville, Gabon.
authors.forename: Jean-Bernard
authors.initials: JB
authors.lastname: Lekana-Douki
authors.affiliation: FRE 3206 CNRS MCAM, Museum National d'Histoire Naturelle, Département Régulations, Développement, Diversité Moléculaire, CP 52, 61 rue Buffon, 75231 Paris Cedex 05, France.
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Mouray
authors.affiliation: Université Lille Nord de France, Université de Lille 1, Unité de Catalyse et de Chimie du Solide, UMR CNRS 8181, ENSCL, B.P. 108, 59652 Villeneuve d'Ascq, France.
authors.forename: Till
authors.initials: T
authors.lastname: Bousquet
authors.affiliation: FRE 3206 CNRS MCAM, Museum National d'Histoire Naturelle, Département Régulations, Développement, Diversité Moléculaire, CP 52, 61 rue Buffon, 75231 Paris Cedex 05, France.
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.affiliation: Université Lille Nord de France, Université de Lille 1, Unité de Catalyse et de Chimie du Solide, UMR CNRS 8181, ENSCL, B.P. 108, 59652 Villeneuve d'Ascq, France.
authors.forename: Sylvain
authors.initials: S
authors.lastname: Pellegrini
authors.affiliation: Centre International de Recherches Médicales de Franceville (CIRMF), Unité de Parasitologie, BP 769 Franceville, Gabon.
authors.forename: Fousseyni Samba
authors.initials: FS
authors.lastname: Toure Ndouo
authors.affiliation: Université des Sciences et Techniques de Masuku, BP 901 Franceville, Gabon. Electronic address: jlebibi@hotmail.com.
authors.forename: Jacques
authors.initials: J
authors.lastname: Lebibi
authors.affiliation: Université Lille Nord de France, Université de Lille 1, Unité de Catalyse et de Chimie du Solide, UMR CNRS 8181, ENSCL, B.P. 108, 59652 Villeneuve d'Ascq, France. Electronic address: lydie.pelinski@univ-lille1.fr.
authors.forename: Lydie
authors.initials: L
authors.lastname: Pélinski
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005296:Ferrous Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D005296:Ferrous Compounds; D011804:Quinolines; C000601780:ferrocenyl aminoquinoline
keywords: Antimalarial assay; Cytotoxicity; Ferrocene; Quinoline