Hoffmeister Björn R, Hejl Michaela, Adib-Razavi Mahsa S, Jakupec Michael A, Galanski Markus, Keppler Bernhard K
Institute of Inorganic Chemistry, University of Vienna, Waehringer Strasse 42, AT-1090 Vienna (phone: +43-1-427752600; fax: +43-1-427752680).
Chem Biodivers. 2015 Apr;12(4):559-74. doi: 10.1002/cbdv.201400291.
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 (1) H-, (13) C-, (15) N-, and (195) Pt-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.
合成了一系列十二个新型二氨四（羧基）铂（IV）和18个新型双（羧基）二氯（乙烷-1,2-二胺）铂（IV）配合物，其轴向羧基配体为混合型，并通过多核（1）H-、（13）C-、（15）N-和（195）Pt-NMR光谱进行了表征。通过MTT法评估了它们对三种源自卵巢畸胎癌（CH1/PA-1）、肺癌（A549）和结肠癌（SW480）的人类癌细胞系的细胞毒性潜力。在对顺铂敏感的CH1/PA-1癌细胞系中，二氨四（羧基）铂（IV）配合物的IC50值处于低微摩尔范围，而对于双（羧基）二氯（乙烷-1,2-二胺）铂（IV）系列中最具亲脂性的化合物，发现其IC50值处于纳摩尔范围。
