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ISBN: 978-83-60043-10-3 - eurobic9

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Eurobic9, 2-6 September, 2008, Wrocław, Poland<br />

P72. Functionalized Cytotoxic Ruthenium(II) Arene Complexes<br />

A. Habtemariam a , P.C.A. Bruijnincx b , P.J. Sadler b<br />

a Chemistry, University of Warwick, Gibett Hill Road, CV4 7AL, Coventry, United Kingdom<br />

e-mail: a.habtemariam@warwick.ac.uk<br />

b Chemistry, University of Warwick, Gibett Hill Road, CV4 7AL, Coventry, United Kingom<br />

Organometallic half-sandwich Ruthenium(II) arenes of the type [(η6- arene)Ru(YZ)(X)]+ where YZ is<br />

typically a chelating diamine ligand (e.g. ethylenediamine, en) and X is a halide (e.g. Cl) exhibit anticancer<br />

activity in vitro and in vivo.[1, 2]<br />

A number of design features are inherent in these classes of compounds. Systematic variations of the<br />

coordinated arene, and the mono- and bidentate ligands can result in complexes having preselected, desirable<br />

features. A number of organometallic Ru(II) arene complexes bearing versatile functional groups, are being<br />

synthesised in our laboratory with a view to generate bimetallic and hetero-bimetallic complexes. In addition<br />

these transformations may enable us to explore the possibility of tuning the selectivity of the compounds in their<br />

interaction with biomolecules by attaching an appropriate probe. The inclusion of specific markers such as<br />

fluorescent dyes may aid in studies of the biodistribution of complexes. The results of these studies will be<br />

discussed in this presentation.<br />

Acknowledgement: We thank NWO (fellowship for PCAB for support and members of COST Action D39 for<br />

discussion.<br />

References:<br />

[1] Habtemariam, A., Melchart, M., Fernandez, R., Parsons, S., Oswald, I. D. H., Parkin, A., Fabbiani, F. P. A.,<br />

Davidson, J. E., Dawson, A., Aird, R. E., Jodrell, D. I., Sadler, P. J. (2006) J. Med. Chem. 49, 6858-6868.<br />

[2] Yan, Y. K., Melchart, M., Habtemariam, A., Sadler, P. J. (2005) Chem. Commun., 4764-4776.<br />

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