Reis, João Paulo BarolliCorrea, Rodrigo de SouzaMiranda, Fabio da SilvaRibeiro, Juliana UemaBloch Junior, CarlosEllena, Javier AlcidesMoreno, VirtudesCominetti, Márcia ReginaBatista, Alzir Azevedo2018-10-152018-10-152017REIS, J. P. B. et al. Polypyridyl ruthenium complexes : novel DNA-intercalating agents against human breast tumor. Journal of the Brazilian Chemical Society, São Paulo, v. 28, n. 10, p. 1879-1889, out. 2017. Disponível em: <http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532017001001879>. Acesso em: 05 abr. 2018.16784790http://www.repositorio.ufop.br/handle/123456789/10368This paper describes a new series of four DNA-intercalating agents with promising anticancer activities, based on ruthenium(II) with the planar ligand dpqQX (dpqQX = dipyrido[3,2-a:2',3'-c]quinoxaline[2,3-b]quinoxaline). The complexes identified as trans-[RuCl2(dppb)(dpqQX)], cis-[RuCl2(dppb)(dpqQX)], ct-[RuCl(CO)(dppb)(dpqQX)]PF6 and ct-[RuCl2(PPh3)2(dpqQX)] (dppb = 1,4-bis(diphenylphosphine)butane and PPh3 = triphenylphosphine) were characterized by 31P{1H} nuclear magnetic resonance (NMR) and infrared spectroscopies, cyclic voltammetry, molar conductance measurements, elemental analysis, mass spectrometry and X-ray diffraction analysis for complex ct-[RuCl2(PPh3)2(dpqQX)]. Their in vitro cytotoxic activities against MDA-MB-213 and MCF-7 breast cancer cells were evaluated and compared with normal L-929 cells. Low drug concentration at which 50% of the cells are viable relative to the control (IC50) values were obtained for all four complexes compared with a reference metallodrug, cisplatin. In addition, DNA affinity studies from titrations, as well as the images obtained by atomic force microscopy (AFM) involving pBR322 plasmid DNA, suggest interactions between the metal complexes and the DNA macromolecule, in which they act as intercalating agents. The intercalation of the complexes with DNA was confirmed by viscosity measurements.en-USabertoMetallo-intercalatorTumor cellsDNA interactionCytotoxicityPolypyridyl ruthenium complexes : novel DNA-intercalating agents against human breast tumor.Artigo publicado em periodicoTodo o conteúdo do periódico Journal of the Brazilian Chemical Society, exceto onde identificado, está licenciado sob uma licença Creative Commons 4.0 que permite copiar, distribuir e transmitir o trabalho em qualquer suporte ou formato desde que sejam citados o autor e o licenciante. Fonte: Journal of the Brazilian Chemical Society <http://www.scielo.br/scielo.php?script=sci_serial&pid=0103-5053&lng=en&nrm=iso>. Acesso em: 02 jan. 2017.