DNA interaction and cytotoxicity studies of new ruthenium(II) cyclopentadienyl derivative complexes containing heteroaromatic ligands |
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Authors: | Moreno Virtudes Font-Bardia Mercè Calvet Teresa Lorenzo Julia Avilés Francesc X Garcia M Helena Morais Tânia S Valente Andreia Robalo M Paula |
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Institution: | a Department de Química Inorgànica, Universitat de Barcelona, Martí y Franquès 1-11, 08028, Barcelona, Spainb Cristal.lografia, Mineralogia i Dipòsits Minerals, Universitat de Barcelona, Martí y Franquès s/n, 08028, Barcelona, Spainc Departamento de Engenharia Química, Instituto Superior de Engenharia de Lisboa, Rua Conselheiro Emídio Navarro, 1, 1959-007 Lisboa, Centro de Química Estrutural, Complexo I, IST, Av. Rovisco Pais, 1049-001 Lisboa, Portugald Centro de Ciências Moleculares e Materiais, Faculdade de Ciências da Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugale Institut de Biotecnologia i de Biomedicina, Universitat Autònoma de Barcelona, 08193, Bellaterra, Barcelona, Spain |
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Abstract: | Four ruthenium(II) complexes with the formula Ru(η5-C5H5)(PP)L]CF3SO3], being (PP = two triphenylphosphine molecules), L = 1-benzylimidazole, ; (PP = two triphenylphosphine molecules), L = 2,2′bipyridine, ; (PP = two triphenylphosphine molecules), L = 4-Methylpyridine, ; (PP = 1,2-bis(diphenylphosphine)ethane), L = 4-Methylpyridine, , were prepared, in view to evaluate their potentialities as antitumor agents. The compounds were completely characterized by NMR spectroscopy and their crystal and molecular structures were determined by X-ray diffraction. Electrochemical studies were carried out giving for all the compounds quasi-reversible processes. The images obtained by atomic force microscopy (AFM) suggest interaction with pBR322 plasmid DNA. Measurements of the viscosity of solutions of free DNA and DNA incubated with different concentrations of the compounds confirmed this interaction. The cytotoxicity of compounds 1234 was much higher than that of cisplatin against human leukemia cancer cells (HL-60 cells). IC50 values for all the compounds are in the range of submicromolar amounts. Apoptotic death percentage was also studied resulting similar than that of cisplatin. |
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Keywords: | Ruthenium (II) Cyclopentadienyl derivatives X-ray structures Antiproliferative assays |
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