Synthesis and Characterization of Platinum(II) Oxadiazoline Complexes and their In Vitro Antitumor Activity in Platinum-Sensitive and -Resistant Cancer Cell Lines | Zendy

Helen M. Coley | Zendy; Julien Sarju | Zendy; Gabriele Wagner | Zendy

Open Access

Synthesis and Characterization of Platinum(II) Oxadiazoline Complexes and their In Vitro Antitumor Activity in Platinum-Sensitive and -Resistant Cancer Cell Lines

Author(s) -

Helen M. Coley,

Julien Sarju,

Gabriele Wagner

Publication year - 2007

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm061263s

Subject(s) - chemistry , platinum , in vitro , cell culture , cancer cell lines , platinum compounds , cancer , cancer cell , biochemistry , stereochemistry , combinatorial chemistry , genetics , catalysis , biology

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 IC 50 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.

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