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In vitro antitumor activity and interaction with DNA model bases of cis-[PtCl2(iPram)(azole)] complexes and comparison with their trans analogues |
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| Authors: | Elena Pantoja Steven van Zutphen Anthony L Spek Jan Reedijk |
| Institution: | a Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, P.O. Box 9502, 2300 RA, Leiden, The Netherlands b Utrecht University, Crystal and Structural Chemistry, Padualaan 8, 3584 CH, Utrecht, The Netherlands c Departamento de Química Inorgánica, Universidad Autónoma de Madrid, Crtra de Colmenar Viejo Km. 15, 28049 Madrid, Spain |
| Abstract: | Asymmetric cis-platinum(II) complexes with isopropylamine and two different azole ligands were synthesized and characterized with different techniques. In addition, for one of the complexes the X-ray structure was determined. Cytotoxicity tests using several human tumor cell lines, including the cisplatin-sensitive cell line A2780 and its cisplatin-resistant analogue. These results were compared with the results obtained for the trans isomers of the presented complexes and a relation between the structure and the activity was established. It was found that complexes with cis geometry are less active than their trans analogues, in particular in the resistant cell line A2780R. However, complex 1 can overcome cisplatin resistance to a certain extent. In the interaction with GMP, the asymmetric cis-Pt(II) complexes react with similar rates as their trans analogues and they behave as bifunctional species. |
| Keywords: | Platinum(II) Planar ligands Amines Cytotoxic activity DNA model bases |
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