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Chem Biodivers. 2019 Jan;16(1):e1800373. doi: 10.1002/cbdv.201800373. Epub 2019 Jan 11.

Platinum(II) Complexes with 1,10-Phenanthroline and Hydrophilic Alkoxyacetate Ligands as Potential Antitumor Agents.

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School of Chemistry, Biology and Materials Engineering, Suzhou University of Science and Technology, Suzhou, 215009, P. R. China.


Four platinum complexes, formulated as [Pt(phen)(OCOCH2 OR)2 ] (phen=1,10-phenanthroline, R=Me, Et, i Pr, or t Bu), have been synthesized and well characterized by elemental analysis, IR, 1 H-NMR, 13 C-NMR and ESI-MS spectroscopy. Replacing chloride groups of the precursor Pt(phen)Cl2 with alkoxyacetate anions greatly improved the aqueous solubility and cytotoxicity of the resulting platinum complexes. The in vitro cytotoxicity study revealed that complexes 1-3 were active in vitro towards four human tumor cell lines, especially complex 1 which exhibited prominent in vitro cytotoxic activity against HCT-116 cell lines comparable to cisplatin and oxaliplatin. Flow cytometry assay indicated that representative complexes 1 and 2 exerted cytotoxicity on HCT-116 cell lines through inducing cell apoptosis and blocking cell cycle progression in the S or G2/M phases. The interaction of representative complexes with pET28a plasmid DNA was tested by agarose gel electrophoresis, which demonstrated that complexes 1 and 2 were capable of distorting plasmid DNA mainly by covalent binding and degradation effect.


1,10-phenanthroline; alkoxyacetates; biological activity; cytotoxicity; flow cytometry; platinum(II) complexes

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