title: Investigation on the pharmacological profile of antimony(III) complexes with hydroxyquinoline derivatives: anti-trypanosomal activity and cytotoxicity against human leukemia cell lines.
abstract: Complexes [Sb(QN)(2)Cl] (1), [Sb(QC)(2)Cl] (2) and [Sb(QI)(2)Cl] (3) were obtained with 8-hydroxyquinoline (HQN), 5-chloro-8-hydroxyquinoline (HQC) and 5-chloro-7-iodo-8-hydroxyquinoline (clioquinol, HQI). The quinoline derivatives and their antimony(III) complexes were evaluated for their anti-trypanosomal activity as well as for their cytotoxicity against HL-60 and Jurkat human leukemia cell lines. Upon coordination to antimony(III) the anti-trypanosomal activity of HQC and HQI increases, the highest improvement being observed for complex (3), which was the most active among all studied compounds against both epimastigote and trypomastigote forms of Trypanosoma cruzi. All quinoline derivatives proved to be cytotoxic against both leukemia cell lineages. Upon coordination to antimony(III) the cytotoxicity of HQN improved against Jurkat leukemia cells. While SbCl(3) proved to be cytotoxic against HL-60 cells, it was not active against Jurkat cells. However, its coordination to the quinoline derivatives resulted in complexes with significant cytotoxicity against Jurkat cells.
authors.affiliation: Departamento de Química, Universidade Federal de Minas Gerais, Belo Horizonte, MG 31270-901, Brazil.
authors.forename: Débora C
authors.initials: DC
authors.lastname: Reis
authors.forename: Mauro C X
authors.initials: MC
authors.lastname: Pinto
authors.forename: Elaine M
authors.initials: EM
authors.lastname: Souza-Fagundes
authors.forename: Lucas F
authors.initials: LF
authors.lastname: Rocha
authors.forename: Valéria R A
authors.initials: VR
authors.lastname: Pereira
authors.forename: Cristiane M L
authors.initials: CM
authors.lastname: Melo
authors.forename: Heloisa
authors.initials: H
authors.lastname: Beraldo
mesh_terms: D000818:Animals; D000965:Antimony / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D006912:Hydroxyquinolines / Q000737:chemistry*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D013154:Spleen / Q000166:cytology / Q000187:drug effects; D013329:Structure-Activity Relationship; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D006912:Hydroxyquinolines; D009942:Organometallic Compounds; D000965:Antimony