Author | Firmino, Gisele S. S. | |
Author | Souza, Marcus V. N. de | |
Author | Pessoa, Claudia | |
Author | Lourenco, Maria C. S. | |
Author | Resende, Jackson A. L. C. | |
Author | Lessa, Josane A. | |
Access date | 2019-02-19T11:45:41Z | |
Available date | 2019-02-19T11:45:41Z | |
Document date | 2016 | |
Citation | FIRMINO, Gisele S. S. et al. Synthesis and evaluation of copper(II) complexes with isoniazid-derived hydrazones as anticancer and antitubercular agents. Biometals, v. 29, p. 953–963, 2016. | pt_BR |
ISSN | 0966-0844 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/31728 | |
Language | eng | pt_BR |
Publisher | Springer Verlag | pt_BR |
Rights | open access | pt_BR |
Title | Synthesis and evaluation of copper(II) complexes with isoniazid-derived hydrazones as anticancer and antitubercular agents | pt_BR |
Type | Article | pt_BR |
DOI | 10.1007/s10534-016-9968-7 | |
Abstract | In this study, the N,N,O metal chelator 2-pyridinecarboxaldehydeisonicotinoyl hydrazone (HPCIH, 1) and its derivatives 2-acetylpyridine-(HAPIH 2), 2-pyridineformamide-(HPAmIH, 3) and pyrazineformamide-(HPzAmIH, 4) were employed in the synthesis of four copper(II) complexes, [Cu(HPCIH)Cl2]·0.4H2O (5), [Cu(HAPIH)Cl2]·1.25H2O (6), [Cu(HPAmIH)Cl2]·H2O (7) and [Cu(HPzAmIH)Cl2]·1.25H2O (8). The compounds were assayed for their action toward Mycobacterium tuberculosis H37Rv ATCC 27294 strain and the human tumor cell lines OVCAR-8 (ovarian cancer), SF-295 (glioblastoma multiforme) and HCT-116 (colon adenocarcinoma). All copper(II) complexes were more effective in reducing growth of HCT-116 and SF-295 cells than the respective free hydrazones at 5 µg/mL, whereas only complex 7 was more cytotoxic toward OVCAR-8 lines than its ligand HPAmIH. 6 proved to be cytotoxic at submicromolar doses, whose IC50 values (0.39-0.86 µM) are similar to those ones found for doxorubicin (0.23-0.43 µM). Complexes 5 and 6 displayed high activity against M. tuberculosis (MIC = 0.85 and 1.58 µM, respectively), as compared with isoniazid (MIC = 2.27 µM), which suggests the compounds are attractive candidates as antitubercular drugs. | pt_BR |
Affilliation | Universidade do Estado do Rio de Janeiro. Instituto de Química. Departamento de Química Geral e Inorgânica. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ , Brasil. | pt_BR |
Affilliation | Universidade Federal do Ceará. Laboratório de Oncologia Experimental. Fortaleza, CE, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal do Mato Grosso. Centro Universitário do Araguaia. Instituto de Ciências Exatas e da Terra. Barra do Garças, MT, Brazil | pt_BR |
Affilliation | Universidade do Estado do Rio de Janeiro. Instituto de Química. Departamento de Química Geral e Inorgânica. Rio de Janeiro, RJ, Brasil. | pt_BR |
Subject | Copper(II) complexes | pt_BR |
Subject | Hydrazones | pt_BR |
Subject | Isoniazid | pt_BR |
Subject | Anticancer agent | pt_BR |
Subject | Antitubercular agent | pt_BR |
e-ISSN | 1572-8773 | |
Embargo date | 2020-01-31 | |