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Synthesis,characterization, DNA binding studies and in vitro cytotoxicity of platinum(II)-dihalogenido complexes containing bidentate chelating N-donor ligands
Authors:Radka K?ikavová  Ján Van?o  Tomá? ?ilha  Jaromír Marek
Institution:Faculty of Science, Department of Inorganic Chemistry, Palacky University, Olomouc, Czech Republic
Abstract:Platinum(II) complexes, Pt(Lx)X2] (16), where X = Br or I and Lx = 2,2′-bipyridine or 1,10-phenanthroline derivatives (5,5′-dimethyl-2,2′-bipyridine (5-Mebpy), 4,4′-dimethyl-2,2′-bipyridine (4-Mebpy), and 5-amino-1,10-phenanthroline (5-NH2phen)) were prepared. The complexes were characterized by the elemental analysis, mass spectrometry, infrared, and multinuclear (1H, 13C and 195Pt) 1-D and 2-D NMR spectroscopies, and by single-crystal X-ray analysis of Pt(4-Mebpy)I2] (4). All the platinum(II) complexes (16) were evaluated for in vitro cytotoxicity against human cancer cell lines A2780 and A2780R, and against non-malignant MRC5 cell line. All the complexes were nontoxic up to the 50 μM concentration, although they were found to readily bind to calf-thymus DNA (CT-DNA), as determined by spectrophotometric titration (Kb ≈ 107 M?1) and ethidium bromide displacement assay.
Keywords:Platinum(II) complexes  2  2′-bipyridine derivatives  1  10-phenanthroline derivatives  in vitro cytotoxicity  CT-DNA  crystal structure
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