Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/31728
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dc.contributor.authorFirmino, Gisele S. S.
dc.contributor.authorSouza, Marcus V. N. de
dc.contributor.authorPessoa, Claudia
dc.contributor.authorLourenco, Maria C. S.
dc.contributor.authorResende, Jackson A. L. C.
dc.contributor.authorLessa, Josane A.
dc.date.accessioned2019-02-19T11:45:41Z
dc.date.available2019-02-19T11:45:41Z
dc.date.issued2016
dc.identifier.citationFIRMINO, 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.
dc.identifier.issn0966-0844
dc.identifier.urihttps://www.arca.fiocruz.br/handle/icict/31728
dc.language.isoeng
dc.publisherSpringer Verlag
dc.rightsrestricted access
dc.titleSynthesis and evaluation of copper(II) complexes with isoniazid-derived hydrazones as anticancer and antitubercular agents
dc.typeArticle
dc.identifier.doi10.1007/s10534-016-9968-7
dc.description.abstractenIn 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.
dc.creator.affilliationUniversidade do Estado do Rio de Janeiro. Instituto de Química. Departamento de Química Geral e Inorgânica. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ , Brasil.
dc.creator.affilliationUniversidade Federal do Ceará. Laboratório de Oncologia Experimental. Fortaleza, CE, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationUniversidade Federal do Mato Grosso. Centro Universitário do Araguaia. Instituto de Ciências Exatas e da Terra. Barra do Garças, MT, Brazil
dc.creator.affilliationUniversidade do Estado do Rio de Janeiro. Instituto de Química. Departamento de Química Geral e Inorgânica. Rio de Janeiro, RJ, Brasil.
dc.subject.enCopper(II) complexes
dc.subject.enHydrazones
dc.subject.enIsoniazid
dc.subject.enAnticancer agent
dc.subject.enAntitubercular agent
dc.identifier.eissn1572-8773
Appears in Collections:Farmanguinhos - Artigos de Periódicos
INI - Artigos de Periódicos

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