title: Evaluation of the trypanocidal, cytotoxic and genotoxic activity of styrylquinoline analogs.
abstract: Styrylquinolines isolated from Galipea longiflora have shown leishmanicidal, trypanocidal, nematocidal and antimalarial activity. Here, we propose to use analogs of these styrylquinolines to enhance the activity against Trypanosoma cruzi. Three compounds in a reduced and oxidized state were synthesized, and the activity against epimastigotes and trypomastigotes was evaluated. in addition, the cytotoxic activity and genotoxic effect were also determined. The results indicated that epimastigotes from different T. cruzi I stocks were highly sensitive to the three compounds. The PQM4 compound presented promising activity against trypomastigotes and low cytotoxic and genotoxic effects. Finally, we observed that the doublebond reduction of the lateral chain of the three carbons made on these compounds improved the activity and substantially diminished the toxicity of the compounds.
authors.affiliation: Grupo Biologia y Control de Enfermedades Infecciosas, Universidad de Antioquia, Medellin, Colombia.
authors.forename: P
authors.initials: P
authors.lastname: García
authors.forename: C
authors.initials: C
authors.lastname: Genes
authors.forename: P
authors.initials: P
authors.lastname: Molano
authors.forename: O
authors.initials: O
authors.lastname: Torres
authors.forename: J
authors.initials: J
authors.lastname: Saez
authors.forename: O
authors.initials: O
authors.lastname: Triana
mesh_terms: D049109:Cell Proliferation / Q000187:drug effects*; D014355:Chagas Disease / Q000235:genetics / Q000469:parasitology; D004249:DNA Damage; D016054:DNA, Protozoan / Q000187:drug effects*; D006801:Humans; D021261:Parasitic Sensitivity Tests; D011804:Quinolines / Q000138:chemical synthesis / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000235:genetics; D020298:U937 Cells
chemical_list: D016054:DNA, Protozoan; D011804:Quinolines; D014344:Trypanocidal Agents; C481600:styrylquinoline