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

Coley, HM, Sarju, J and Wagner, G (2008) Synthesis and characterization of platinum(II) oxadiazoline complexes and their in vitro antitumor activity in platinum-sensitive and -resistant cancer cell lines JOURNAL OF MEDICINAL CHEMISTRY, 51 (1). 135 - 141. ISSN 0022-2623

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Abstract

A series of platinum(II) complexes bearing Δ4-1,2,4-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.

Item Type: Article
Additional Information: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher.To access the final edited and published work see http://dx.doi.org/10.1021/jm061263s.
Uncontrolled Keywords: Science & Technology, Life Sciences & Biomedicine, Chemistry, Medicinal, Pharmacology & Pharmacy, OVARIAN-CANCER, TRANS-PLATINUM(II) COMPLEXES, BOUND ORGANONITRILES, APOPTOSIS INDUCTION, BIOLOGICAL-ACTIVITY, 2+3 CYCLOADDITION, PLANAR LIGANDS, NITRONES, CYTOTOXICITY, COORDINATION
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Divisions: Faculty of Health and Medical Sciences > Biochemistry and Physiology
Depositing User: Symplectic Elements
Date Deposited: 29 Jun 2012 10:53
Last Modified: 23 Sep 2013 19:32
URI: http://epubs.surrey.ac.uk/id/eprint/711611

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