title: [Styrylquinolines-type synthetic compounds with leishmanicidal and cytotoxic activities].
abstract: BACKGROUND
  Leishmaniasis is a major public health problem faced by many countries, including Colombia. Its treatment has limitations such as the toxicity of the drugs used, the emergence of resistant strains, and prolonged and expensive treatments. Thus, there is an urgent need to find alternative solutions.
  
  
  OBJECTIVE
  To evaluate the leishmanicidal and cytotoxic activities of three 2-styrylquinolines type compounds: 2-[(E)-2-(2,3-diacetyloxyphenyl)ethenyl]quinolin-8-yl-acetate, E1; 2-[(E)-2-(4-acetyloxy-3-methoxyphenyl)ethenyl] quinoline, E2, and 2-[(E)-2-(2,3-diacetyloxyphenyl)ethenyl] quinoline, E3.
  
  
  METHODS
  The 2-styrylquinolines were obtained by organic synthesis using Perkin-type condensation reaction from 8-hydroxy quinaldine or quinaldine and aromatic aldehydes. The leishmanicidal activity was evaluated on intracellular amastigotes of Leishmania (Viannia) panamensis by flow cytometry. The results were expressed as lethal concentration 50 (LC 50 ) for cytotoxicity and effective concentration 50 (EC 50 ) for leishmanicidal activity, calculated by the Probit method.
  
  
  RESULTS
  E3 showed high activity against L. (V) panamensis with a calculated EC 50 value of 1.4 µg/ml, and a selectivity index of 3.9; E1 and E2 showed higher EC 50 values of 5.6 and 68.1 µg/ml, respectively. For cytotoxicity, LC 50 values ranging from 5.4 to 68.1 µg/ml were calculated. E2 was moderately toxic, showing an LC 50 very similar to that of amphotericin B, a substance used as cytotoxic control.
  
  
  CONCLUSIONS
  The styrylquinoline E3 is a promising compound against L. (V) panamensis , as it was able to significantly inhibit amastigotes inside the cell, reducing infection despite its toxicity.
authors.affiliation: Grupo de Investigación en Química de los Productos Naturales, Facultad de Ciencias Básicas, Universidad de Córdoba, Montería, Colombia.
authors.forename: Emy Luz
authors.initials: EL
authors.lastname: Sánchez
authors.affiliation: Grupo de Investigación en Química de los Productos Naturales, Facultad de Ciencias Básicas, Universidad de Córdoba, Montería, Colombia.
authors.forename: Gílmar Gabriel
authors.initials: GG
authors.lastname: Santafé
authors.affiliation: Grupo de Investigación en Desarrollo y Evaluación de Fármacos y Afines, IDEFARMA, Facultad de Ciencias de la Salud, Universidad de Córdoba.
authors.forename: Omar Leonardo
authors.initials: OL
authors.lastname: Torres
authors.affiliation: Programa de Estudio y Control de Enfermedades Tropicales, PECET, Instituto de Investigaciones Médicas, Facultad de Medicina, Universidad de Antioquia.
authors.forename: Diana Lorena
authors.initials: DL
authors.lastname: Muñoz
authors.affiliation: Centro para el Desarrollo de Productos, CIDEPRO, Medellín, Colombia.
authors.forename: Sara María
authors.initials: SM
authors.lastname: Robledo
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D006801:Humans; D018334:Leishmania guyanensis / Q000187:drug effects*; D007928:Lethal Dose 50; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013343:Styrenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D020298:U937 Cells / Q000187:drug effects*
chemical_list: C000600439:2-(2-(2,3-diacetyloxyphenyl)ethenyl)quinolin-8-yl acetate; C000600441:2-(2-(2,3-diacetyloxyphenyl)ethenyl)quinoline; C000600440:2-(2-(4-acetyloxy-3-methoxyphenyl)ethenyl)quinoline; D000981:Antiprotozoal Agents; D011804:Quinolines; D013343:Styrenes; C481600:styrylquinoline