Bis‐ and Tetrakis(carboxylato)platinum(IV) Complexes with Mixed Axial Ligands – Synthesis,Characterization, and Cytotoxicity |
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| Authors: | Björn R. Hoffmeister Michaela Hejl Mahsa S. Adib‐Razavi Michael A. Jakupec Markus Galanski Bernhard K. Keppler |
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| Affiliation: | 1. Institute of Inorganic Chemistry, University of Vienna, Waehringer Strasse 42, AT‐1090?Vienna (phone: +43‐1‐427752600;2. fax: +43‐1‐427752680);3. Research Platform ‘Translational Cancer Therapy Research', University of Vienna, Waehringer Strasse 42, AT‐1090 Vienna |
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| Abstract: | A series of twelve novel diamminetetrakis(carboxylato)platinum(IV) and 18 novel bis(carboxylato)dichlorido(ethane‐1,2‐diamine)platinum(IV) complexes with mixed axial carboxylato ligands was synthesized and characterized by multinuclear 1H‐, 13C‐, 15N‐, and 195Pt‐NMR spectroscopy. Their cytotoxic potential was evaluated (by MTT assay) against three human cancer cell lines derived from ovarian teratocarcinoma (CH1/PA‐1), lung (A549), and colon carcinoma (SW480). In the cisplatin‐sensitive CH1/PA‐1 cancer cell line, diamminetetrakis(carboxylato)platinum(IV) complexes showed IC50 values in the low micromolar range, whereas, for the most lipophilic compounds of the bis(carboxylato)dichlorido(ethane‐1,2‐diamine)platinum(IV) series, IC50 values in the nanomolar range were found. |
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| Keywords: | Platinum complexes 195Pt‐NMR Spectroscopy Cytotoxic activity |
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