gms | German Medical Science

27th German Cancer Congress Berlin 2006

German Cancer Society (Frankfurt/M.)

22. - 26.03.2006, Berlin

Cytotoxicity of enantiomerically pure [1,2-diamino-1-phenyl-2-alkylethane]dichloroplatin(II) complexes on different cancer cell lines

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27. Deutscher Krebskongress. Berlin, 22.-26.03.2006. Düsseldorf, Köln: German Medical Science; 2006. DocPO008

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Published: March 20, 2006

© 2006 Dullin.
This is an Open Access article distributed under the terms of the Creative Commons Attribution License ( You are free: to Share – to copy, distribute and transmit the work, provided the original author and source are credited.



Since the discovery of Cisplatin numerous platinum complexes have been synthesized and tested for antitumor activity. In order to overcome the disadvantages of Cisplatin, the NH3 ligands were exchanged by an 1,2-Diaryl- or 1-Aryl-2-Alkyl-rest showed high activity against the MCF-7 and the MDA-MB 231 breast cancer cell line as well on the LNCaP/FGC prostate cancer cell line [1]. The most active ones were out of the [1-Aryl-2-Alkyl]series with a 4-F- substituent in the aromatic ring [2]. In various studies the complexes showed stereoselectivity: the D,L complexes are more active than the meso ones. In order to demonstrate if a significant enantioselectivity exist we synthesized 1-Aryl-2-Alkyl with long and branched hydrocarbon chain to increase lipophilicity , the cytotoxic activity were evaluated on mammacarcinome and prostate cancer cell lines. The complexes with an ethyl- and isopropyl chain were the most active ones. The configuration determined the antitumor effects, dependently on the cell line used: MCF-7: RR>SS>RS>SR; MDA-MB 231: SS>RR>RS=SR; LNCaP/FGC: SS>RR>RS>SR. The role of isopropyl group for stereochemical discrimination between the isomers was shown.


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