title: Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines.
abstract: A series of original 4-aryl-substituted 2-trichloromethylquinazoline derivatives was synthesized using a microwave-assisted Suzuki-Miyaura cross-coupling approach. Antiplasmodial activity was evaluated on both chloroquino-resistant and -sensitive Plasmodium falciparum strains, and the selectivity indexes for THP1 and HepG2 human cells were also calculated, revealing their antiplasmodial potential.
authors.affiliation: Laboratoire de Chimie Organique Pharmaceutique, UMR CNRS 6517, Faculté de Pharmacie, Université de la Méditerranée, 27 Bd. Jean Moulin, 13385 Marseille Cedex 05, France.
authors.forename: Pierre
authors.initials: P
authors.lastname: Verhaeghe
authors.forename: Nadine
authors.initials: N
authors.lastname: Azas
authors.forename: Monique
authors.initials: M
authors.lastname: Gasquet
authors.forename: Sébastien
authors.initials: S
authors.lastname: Hutter
authors.forename: Christophe
authors.initials: C
authors.lastname: Ducros
authors.forename: Michèle
authors.initials: M
authors.lastname: Laget
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
authors.forename: Pascal
authors.initials: P
authors.lastname: Rathelot
authors.forename: Patrice
authors.initials: P
authors.lastname: Vanelle
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D006843:Hydrocarbons, Chlorinated / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D010963:Plasmodium falciparum / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000962:Antimalarials; D006843:Hydrocarbons, Chlorinated; D011799:Quinazolines; D002738:Chloroquine