title: Antiplasmodial activities of 4-aminoquinoline-statine compounds.
abstract: We report the discovery of new potent inhibitors of the growth of Plasmodium falciparum chloroquine (CQ)-resistant W2 strain. These compounds were designed using the double drug approach by introducing a residue able to enhance the accumulation of plasmepsins inhibitors into the food vacuole. Some of the molecules were more active than CQ against CQ-resistant strain and showed good selectivity against cathepsin D.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milan, Italy.
authors.forename: Nadia
authors.initials: N
authors.lastname: Vaiana
authors.forename: Melissa
authors.initials: M
authors.lastname: Marzahn
authors.forename: Silvia
authors.initials: S
authors.lastname: Parapini
authors.forename: Peng
authors.initials: P
authors.lastname: Liu
authors.forename: Mario
authors.initials: M
authors.lastname: Dell'Agli
authors.forename: Andrea
authors.initials: A
authors.lastname: Pancotti
authors.forename: Enrico
authors.initials: E
authors.lastname: Sangiovanni
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Basilico
authors.forename: Enrica
authors.initials: E
authors.lastname: Bosisio
authors.forename: Ben M
authors.initials: BM
authors.lastname: Dunn
authors.forename: Donatella
authors.initials: D
authors.lastname: Taramelli
authors.forename: Sergio
authors.initials: S
authors.lastname: Romeo
mesh_terms: D000596:Amino Acids / Q000737:chemistry / Q000494:pharmacology*; D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002402:Cathepsin D / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000634:Aminoquinolines; D000962:Antimalarials; D011480:Protease Inhibitors; D002402:Cathepsin D; C001920:4-aminoquinoline; C013165:statine