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Bioorg Med Chem Lett. 2013 Apr 1;23(7):2117-22. doi: 10.1016/j.bmcl.2013.01.119. Epub 2013 Feb 8.

Synthesis, crystal structures, DNA binding and cytotoxicity of two novel platinum(II) complexes containing 2-(hydroxymethyl)pyridine and pyridine-2-carboxylate ligands.

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Department of Chemistry, Faculty of Arts and Sciences, Uludag University, 16059 Bursa, Turkey.


Two new platinum(II) complexes, trans-[Pt(2-mpy)(2)]·4H(2)O (1) and [PtCl(2-pyc)(2-hmpy)]·H(2)O (2), where 2-hmpy=2-(hydroxymethyl)pyridine, 2-mpy=deprotonated 2-hmpy and 2-pyc=pyridine-2-carboxylate, have been synthesized and characterized by elemental analysis, IR, NMR, and X-ray crystallography. The DNA binding affinities of these complexes for Fish Sperm DNA (FS-DNA) were investigated using fluorescence, viscosity, thermal denaturation and gel electrophoresis measurements. Fluorescence analysis indicates that complex 1 binds to DNA by a single intercalative mechanism, while complex 2 exhibits two types of interactions such as intercalation and covalent binding. Gel electrophoresis assay demonstrates ability of the complexes to cleavage the supercoiled pBR322 plasmid DNA. The in vitro cytotoxicities of both complexes were preliminarily evaluated and the cytotoxicity of complex 1 against the human lung cancer cells (H1299) is similar to oxaliplatin, but higher than transplatin and carboplatin.

[Indexed for MEDLINE]

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