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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Diamminetetrakis(carboxylato)platinum(IV) complexes--synthesis, characterization, and cytotoxicity
Björn R Hoffmeister1, Mahsa S Adib-Razavi, Michael A Jakupec
1University of Vienna, Institute of Inorganic Chemistry, Währinger Strasse 42, AT-1090 Vienna.
Abstract:
A series of eight novel diamminetetrakis(carboxylato)platinum(IV) complexes was synthesized and characterized by multinuclear (1)H-, (13)C-, (15)N-, and (195)Pt-NMR spectroscopy. Their antiproliferative potency was evaluated in three human cancer cell lines representing ovarian (CH1), lung (A549), and colon carcinoma (SW480). In cisplatin-sensitive CH1 cancer cells, cytotoxicity was found in the low micromolar range, whereas, in inherently cisplatin-resistant A549 and SW480 cells, the activity was very low or negligible. Astonishingly, raise in lipophilicity of the complexes, as found in the case of cisplatin analogs, did not result in a significant enhancement of the cytotoxic effect.
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