DNA binding, topoisomerase inhibition and cytotoxicity of palladium(II) complexes with 1,10-phenanthroline and thioureas

dc.contributor.authorBarra, Carolina V. [UNESP]
dc.contributor.authorRocha, Fillipe V.
dc.contributor.authorMorel, Laurent
dc.contributor.authorGautier, Arnaud
dc.contributor.authorGarrido, Saulo S. [UNESP]
dc.contributor.authorMauro, Antonio E. [UNESP]
dc.contributor.authorFrem, Regina C.G. [UNESP]
dc.contributor.authorNetto, Adelino V.G. [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionCiência e Tecnologia
dc.contributor.institutionUniversidade Federal de São Carlos (UFSCar)
dc.contributor.institutionINSERM U931
dc.contributor.institutionUMR 6296
dc.date.accessioned2018-12-11T17:01:47Z
dc.date.available2018-12-11T17:01:47Z
dc.date.issued2016-05-01
dc.description.abstractMetallointercalators represent a promising alternative in cancer chemotherapy. We present herein DNA binding, topoisomerase inhibition and cytotoxic studies on a series of complexes of general formulae [Pd(phen)(tu∗)2]2+ incorporating the intercalator 1,10-phenanthroline and thiourea ligands (L = thiourea 1, N-methylthiourea 2, N,N′-dimethylthiourea 3). DNA-unwinding results showed that the complexes can induce the unwinding of the plasmid DNA. The binding constants (Kb) for the interaction of the complexes with SS-DNA were determined by UV spectroscopy. Competitive experiments with ethidium bromide (EB) were investigated by fluorescence spectroscopy and show that all the complexes were able to displace EB from the DNA-EB complex. The results suggest that they may interact with DNA by intercalation. Compounds were tested against human oral carcinoma cell line (KB), human breast cancer cell line (MCF7) and cisplatin-resistant human breast cancer cell line (MCF7-R) and showed good cytotoxic activity towards MCF7-R. Compounds 2 and 3 were also able to cause topo II inhibition.en
dc.description.affiliationDepartamento de Química Geral e Inorgânica Instituto de Química UNESP
dc.description.affiliationInstituto Federal de Educação Ciência e Tecnologia
dc.description.affiliationDepartamento de Química Universidade Federal de São Carlos
dc.description.affiliationClermont-Université Université Blaise Pascal GreD UMR 6247 CNRS INSERM U931, 24 Avenue des Landais
dc.description.affiliationClermont-Université ICCF Université Blaise Pascal CNRS UMR 6296
dc.description.affiliationDepartamento de Bioquímica e Tecnologia Química Instituto de Química UNESP
dc.description.affiliationUnespDepartamento de Química Geral e Inorgânica Instituto de Química UNESP
dc.description.affiliationUnespDepartamento de Bioquímica e Tecnologia Química Instituto de Química UNESP
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 2014/11340-0
dc.format.extent54-60
dc.identifierhttp://dx.doi.org/10.1016/j.ica.2016.02.053
dc.identifier.citationInorganica Chimica Acta, v. 446, p. 54-60.
dc.identifier.doi10.1016/j.ica.2016.02.053
dc.identifier.file2-s2.0-84960929909.pdf
dc.identifier.issn0020-1693
dc.identifier.lattes7927677053650819
dc.identifier.orcid0000-0002-0057-7964
dc.identifier.scopus2-s2.0-84960929909
dc.identifier.urihttp://hdl.handle.net/11449/172693
dc.language.isoeng
dc.relation.ispartofInorganica Chimica Acta
dc.relation.ispartofsjr0,485
dc.rights.accessRightsAcesso aberto
dc.sourceScopus
dc.subjectCytotoxicity
dc.subjectDNA binding
dc.subjectMetallointercalator
dc.subjectPalladium(II)
dc.subjectThioureas
dc.subjectTopoisomerase inhibitors
dc.titleDNA binding, topoisomerase inhibition and cytotoxicity of palladium(II) complexes with 1,10-phenanthroline and thioureasen
dc.typeArtigo
unesp.author.lattes7927677053650819[8]
unesp.author.lattes3300223970814448[6]
unesp.author.orcid0000-0002-0057-7964[8]

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