Ru(II) complexes containing uracil nucleobase analogs with cytotoxicity against tumor cells.

作者: Rodrigo S Correa , Larissa M Bomfim , Katia M Oliveira , Diogo RM Moreira , Milena BP Soares

DOI: 10.1016/J.JINORGBIO.2019.110751

关键词:

摘要: Abstract We report on chemistry and cytotoxic studies of four new ruthenium (II) complexes containing uracil derivatives. All compounds are neutral, presenting the formula [Ru(PPh 3 ) 2 (2TU) ] ( 1 ), (6m2TU) [Ru(dppb)(2TU) [Ru(dppb)(6m2TU) 4 where PPh  = triphenylphosphine; dppb = 1,4- bis (diphenylphosphino)butane, 2TU = 2-thiouracil 6m2TU = 6-methyl-2-thiouracil. They were characterized using NMR, UV–vis IR spectroscopies, microanalytical analysis mass spectrometry. Furthermore, crystal structures – determined by single-crystal X-ray diffraction. The coordination 2-thiouracil derivatives with increases regions able to carry out hydrogen bonds biological targets, such as DNA. evaluated interaction DNA UV/Vis spectrophotometric titration, a result, values DNA-binding constants in range 0.8–1.8 × 10  M −1 . Moreover, BSA was investigated. In vitro , activities against B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), HL-60 promyelocytic leukemia) K562 chronic myelocytic non-tumor cells: PBMC peripheral blood mononuclear cells activated concanavalin A human lymphoblast) carried out. Cytotoxicity assays revealed that present activity tumor comparable oxaliplatin, reference platinum drug, revealing they promising molecules for developing antitumor compounds.

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