Book of Abstracts - Ruhr-Universität Bochum

P-42
ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum
Characterisation of Zeise´s Salt - Analogues Regarding Cytotoxicity and Stability
Sandra Meieranz a amdRonald Gust *a
a Freie Universität Berlin, Institute of Pharmacy, Königin-Luise-Str. 2+4, 14195 Berlin, Germany.
Platinum complexes are widely used in antitumor therapy. DNA is their main target in cells forming a
covalent bond to the N7 position of guanine. The intolerable side effects and the acquired resistance
during the therapy encouraged the synthesis of new platinum compounds to afford drugs with
improved pharmacological properties and broaden antitumor activity. 1 Therefore, we synthesized
Zeise´s Salts analogues and examined their cytotoxicity in comparison to cisplatin. The complexes
were prepared according to literature procedures. 2 Zeise´s Salt is known as a water stable platinum
complex.
We tested the synthesized compounds on hormone dependent MCF-7 and hormone independent
MDA-MB-231 breast cancer cell lines. The cytotoxicity was very low. Therefore, we determine the
stability in aqueous solution using HPLC and LC-MS. Interestingly, the ester in our compounds is
rapidly cleaved resulting in inactive degradation products. Further investigations on the stability are of
interest to get stabile Zeise´s Salt analogue platinum complexes.
References
1. Wong, E.; Giandomenico, C. M. Chem. Rev. 1999, 99, 2451.
2. Chock, P. B.; Halpern, J.; Paulik, F. E. Inorg. Syn. 1973, 14, 90.
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