Please use this identifier to cite or link to this item:
SYNTHESIS, CHARACTERIZATION, DNA BINDING, DNA CLEAVAGE, PROTEIN BINDING AND CYTOTOXIC ACTIVITIES OF RU(II) COMPLEXES
Author
Affilliation
Abstract in Portuguese
Relatamos a síntese de novos compostos de Ru(II) (Ru-1 a Ru-8) contendo ligantes R-pdc, 4-Cl-pbinh (onde R = 4-CF3, 4-F, 4-OH pdc = 3-fenil-5-(1H-pirrol-2-il)-4,5-di-hidro-1H-pirazol-1-carbotioamida, pbinh = fenoxibenzilideno isonicotinil hidrazidas) e sua atividade antitumoral in vitro em relação às linhagens celulares leucemia murina L1210, linfócitos humanos CEM, carcinoma cervical epitelial humano HeLa, BEL-7402 e Molt4/C8. Alguns dos complexos exibiram atividade antiproliferativa mais potente contra linhagens celulares do que o medicamento padrão cisplatina. O complexo de rutênio Ru-2 apresentou citotoxicidade potente do que a da cisplatina. Propriedades de ligação de DNA, clivagem de DNA e ligação de proteína de complexos de rutênio com esses ligantes são relatadas. Interações desses complexos de rutênio com DNA revelaram um modo intercalativo de ligação entre eles. Espectros de fluorescência síncrona provaram que a interação de complexos de rutênio com albumina de soro bovino (BSA) resultou em uma mudança conformacional desta última.
Abstract
We report on the synthesis of novel Ru(II) compounds (Ru-1 to Ru-8) bearing R-pdc, 4-Cl-pbinh ligands (where R = 4-CF3, 4-F, 4-OH pdc = 3-phenyl-5-(1H-pyrrol-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide, pbinh = phenoxybenzylidene isonicotinyl hydrazides) and their in vitro antitumor activity toward the cell lines murine leukemia L1210, human lymphocyte CEM, human epithelial cervical carcinoma HeLa, BEL-7402 and Molt4/C8. Some of the complexes exhibited more potent antiproliferative activity against cell lines than the standard drug cisplatin. Ruthenium complex Ru-2 displayed potent cytotoxicity with than that of cisplatin. DNA-binding, DNA cleavage and protein binding properties of ruthenium complexes with these ligands are reported. Interactions of these ruthenium complexes with DNA revealed an intercalative mode of binding between them. Synchronous fluorescence spectra proved that the interaction of ruthenium complexes with bovine serum albumin (BSA) resulted in a conformational change of the latter.
Share