title: In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives.
abstract: An in vitro investigation of the antiplasmodial and cytotoxic activities of a series of human choline kinase inhibitors against Plasmodium falciparum is reported. Structure-activity relationship analyses have allowed us to determine the essential parameters for the antimalarial effect of these asymmetrical pyridinium derivatives. One of the compounds meets the World Health Organization's criteria for hit identification against P. falciparum exhibiting an IC50 of 0.0016 μg/ml and a selectivity index of >3000.
authors.affiliation: Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Universidad de Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
authors.forename: Belén
authors.initials: B
authors.lastname: Rubio-Ruiz
authors.affiliation: Instituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Avenida del Conocimiento s/n, 18100 Armilla, Granada, Spain.
authors.forename: Víctor M
authors.initials: VM
authors.lastname: Castillo-Acosta
authors.affiliation: Instituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Avenida del Conocimiento s/n, 18100 Armilla, Granada, Spain.
authors.forename: Guiomar
authors.initials: G
authors.lastname: Pérez-Moreno
authors.affiliation: Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Universidad de Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
authors.forename: Antonio
authors.initials: A
authors.lastname: Espinosa
authors.affiliation: Instituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Avenida del Conocimiento s/n, 18100 Armilla, Granada, Spain.
authors.forename: Dolores
authors.initials: D
authors.lastname: González-Pacanowska
authors.affiliation: Instituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Avenida del Conocimiento s/n, 18100 Armilla, Granada, Spain.
authors.forename: Luis M
authors.initials: LM
authors.lastname: Ruiz-Pérez
authors.affiliation: Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Universidad de Granada, Campus de Cartuja s/n, 18071 Granada, Spain. Electronic address: aentrena@ugr.es.
authors.forename: Antonio
authors.initials: A
authors.lastname: Entrena
authors.affiliation: Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Universidad de Granada, Campus de Cartuja s/n, 18071 Granada, Spain. Electronic address: aconejo@ugr.es.
authors.forename: Ana
authors.initials: A
authors.lastname: Conejo-García
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D006801:Humans; D020128:Inhibitory Concentration 50; D010963:Plasmodium falciparum / Q000187:drug effects*; D011726:Pyridinium Compounds / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats
chemical_list: D000962:Antimalarials; D011726:Pyridinium Compounds
keywords: Antimalarial activity; Cytotoxicity; Plasmodium falciparum; Pyridinium compounds