title: Antiplasmodial activity and cytotoxicity of bis-, tris-, and tetraquinolines with linear or cyclic amino linkers.
abstract: Bisquinoline heteroalkanediamines were structurally modified in order to study the effects of enhanced bulkiness and rigidity on both their activity on strains of Plasmodium falciparum expressing different degrees of chloroquine (CQ) resistance and their cytotoxicity toward mammalian cells. While cyclization yielded molecules of greater rigidity that were not more active than their linear counterparts, they were characterized by an absence of cytotoxicity. Alternatively, dimerization of these compounds led to tetraquinolines that are very potent for CQ-resistant strains and noncytotoxic.
authors.affiliation: UMR CNRS 8525, Université de Lille II, Institut de Biologie et Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447, 59021 Lille Cedex, France.
authors.forename: S
authors.initials: S
authors.lastname: Girault
authors.forename: P
authors.initials: P
authors.lastname: Grellier
authors.forename: A
authors.initials: A
authors.lastname: Berecibar
authors.forename: L
authors.initials: L
authors.lastname: Maes
authors.forename: P
authors.initials: P
authors.lastname: Lemière
authors.forename: E
authors.initials: E
authors.lastname: Mouray
authors.forename: E
authors.initials: E
authors.lastname: Davioud-Charvet
authors.forename: C
authors.initials: C
authors.lastname: Sergheraert
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D002478:Cells, Cultured; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D017737:Macrophages, Peritoneal / Q000187:drug effects; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity
chemical_list: D000962:Antimalarials; D011804:Quinolines; D002738:Chloroquine