University of Vienna, Institute of Inorganic Chemistry, Währinger Strasse 42, AT-1090 Vienna.
Chem Biodivers. 2012 Sep;9(9):1840-8. doi: 10.1002/cbdv.201200019.
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.
一系列八种新型的二氨四（羧酸根）合铂（IV）配合物被合成并通过多核（1）H、（13）C、（15）N 和（195）Pt-NMR 光谱进行了表征。它们的抗增殖活性在三种代表卵巢癌（CH1）、肺癌（A549）和结肠癌（SW480）的人类癌细胞系中进行了评估。在顺铂敏感的 CH1 癌细胞中，细胞毒性在低微摩尔范围内被发现，而在固有顺铂耐药的 A549 和 SW480 细胞中，活性非常低或可忽略不计。令人惊讶的是，正如顺铂类似物的情况一样，配合物亲脂性的提高并没有导致细胞毒性作用的显著增强。
