Synthesis and characterization of platinum(II) oxadiazoline complexes and their in vitro antitumor activity in platinum-sensitive and -resistant cancer cell lines

被引:52
作者
Coley, Helen M. [1 ]
Sarju, Julien [2 ]
Wagner, Gabriele [2 ]
机构
[1] Univ Surrey, Postgrad Med Sch, Guildford GU2 7XH, Surrey, England
[2] Univ Surrey, Div Chem, SBMS, Guildford GU2 7XH, Surrey, England
关键词
D O I
10.1021/jm061263s
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of platinum(II) complexes bearing Delta(4)-1,2,4-oxadiazoline ligands have been synthesized and characterized. Their in vitro antitumor activity has been assessed in platinum-sensitive and -resistant human ovarian cancer cell lines (PEO1, PEOCisR, PEOCarboR, and SK-OV3), as well as in colon cancer (SW948) and testicular cancer cell lines (N-TERA). All compounds tested showed potent cytotoxicity in the platinum-sensitive cell lines and retained activity in the cisplatin- and carboplatin-resistant lines, with IC50 values similar to the parental drug sensitive counterpart. We propose, therefore, that platinum(II) oxadiazoline complexes may possess a novel mechanism of action, which render them active in tumor cells, with resistance to currently used platinum anticancer agents.
引用
收藏
页码:135 / 141
页数:7
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