Book of Abstracts - Ruhr-Universität Bochum

P-07
ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum
Development of Novel [Diarylsalene]- and [Salophene]platinum(II) Complexes
as Cytotoxic Agents
Maria Proetto a amd Ronald Gust *a
a Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Str. 2 + 4, 14195 Berlin, Germany
Breast cancer is the most common cancer in women. 1 Platinum-based drugs are widely used against
various solid tumours, but they are inactive against breast cancer.
In this project, new platinum analogues have been synthesized in an attempt to overcome this problem.
The complexes were tested in vitro for growth inhibitory activity on both hormone dependent MCF-7
(ER+) and hormone independent MDA-MB-231 (ER-) breast cancer cells to determine possible
selective effects.
Based on the experience of the coordination chemistry of Schiff base ligands with different metals,
we chose diarylsalene and salophene as ligands and synthesized two types of platinum complexes
(Figure 1). Variations of the substituents in the aromatic rings were made to evaluate their significance
for the cytotoxic profile. In order to understand the mode of action of these [diarylsalene]platinum(II)
and [salophene]platinum(II) complexes, they were tested in vitro for DNA-binding and DNAintercalation.
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References
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Figure 1
1. World Health Organization International Agency for Research on Cancer. "World Cancer Report"
2003.
2. R. Gust, I. Ott, D. Posselt, K. Sommer, J. Med. Chem. 2004, 47, 5837-5846.
3. A. Hille, I. Ott, A. Kitanovic, I. Kitanovic, H. Alborzina, E. Lederer, S. Wölfl, N. Metzler-Nolte, S.
Schäfer, W.S. Sheldrick, C. Bischof, U. Schatzschneider, R. Gust, J. Biol. Inorg. Chem. 2009, 14, 711-
725.
65
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[diarylsalene]Pt(II) complexes [salophene]Pt(II) complexes
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2, 3