title: Preparation of rotenone derivatives and in vitro analysis of their antimalarial, antileishmanial and selective cytotoxic activities.
abstract: Six derivatives of the known biopesticide rotenone were prepared by several chemical transformations. Rotenone and its derivatives showed differential in vitro antiparasitic activity and selective cytotoxicity. In general, compounds were more active against Plasmodium falciparum than Leishmania panamensis. Rotenone had an EC50 of 19.0 µM against P. falciparum, and 127.2 µM against L. panamensis. Although chemical transformation does not improve its biological profile against P. falciparum, three of its derivatives showed a significant level of action within an adequate range of activity with EC50 values < 50.0 µM. This antiplasmodial activity was not due to red blood cell hemolysis, since LC50 was >>400 µM. On the other hand, all derivatives displayed a non-specific cytotoxicity on several cell lines and primary human cell cultures.
authors.affiliation: PECET, Instituto de Investigaciones Médicas, Facultad de Medicina, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. yulexa1@gmail.com.
authors.forename: Yulieth
authors.initials: Y
authors.lastname: Upegui
authors.affiliation: Grupo Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. juanf.gil@udea.edu.co.
authors.forename: Juan F
authors.initials: JF
authors.lastname: Gil
authors.affiliation: Grupo Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. wiston.quinones@udea.edu.co.
authors.forename: Wiston
authors.initials: W
authors.lastname: Quiñones
authors.affiliation: Grupo Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. fernando.torres@udea.edu.co.
authors.forename: Fernando
authors.initials: F
authors.lastname: Torres
authors.affiliation: Grupo Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. gustavo.escobar1@udea.edu.co.
authors.forename: Gustavo
authors.initials: G
authors.lastname: Escobar
authors.affiliation: PECET, Instituto de Investigaciones Médicas, Facultad de Medicina, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. yulexa1@gmail.com.
authors.forename: Sara M
authors.initials: SM
authors.lastname: Robledo
authors.affiliation: Grupo Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia. feche@une.net.co.
authors.forename: Fernando
authors.initials: F
authors.lastname: Echeverri
mesh_terms: D000962:Antimalarials / Q000494:pharmacology*; D000977:Antiparasitic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007891:Leishmania / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D012402:Rotenone / Q000494:pharmacology*; D020298:U937 Cells
chemical_list: D000962:Antimalarials; D000977:Antiparasitic Agents; D012402:Rotenone