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Open Access research with a European policy impact...

The Strathprints institutional repository is a digital archive of University of Strathclyde's Open Access research outputs. Strathprints provides access to thousands of Open Access research papers by Strathclyde researchers, including by researchers from the European Policies Research Centre (EPRC).

EPRC is a leading institute in Europe for comparative research on public policy, with a particular focus on regional development policies. Spanning 30 European countries, EPRC research programmes have a strong emphasis on applied research and knowledge exchange, including the provision of policy advice to EU institutions and national and sub-national government authorities throughout Europe.

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Structure-activity relationships for cytotoxic ruthenium(II) arene complexes containing N,N-, N,O-, and O,O-chelating ligands

Habtemariam, Abraha and Melchart, Michael and Fernandez, Rafael and Parsons, Simon and Oswald, Iain D. H. and Parkin, Andrew and Fabbiani, Francesca P. A. and Davidson, James E. and Dawson, Alice and Aird, Rhona E. and Jodrell, Duncan I. and Sadler, Peter J. (2006) Structure-activity relationships for cytotoxic ruthenium(II) arene complexes containing N,N-, N,O-, and O,O-chelating ligands. Journal of Medicinal Chemistry, 49 (23). pp. 6858-6868. ISSN 0022-2623

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Abstract

We report structure-activity relationships for organometallic Ru-II complexes of the type [( eta(6)-arene) Ru-( XY) Cl] Z, where XY is an N, N-( diamine), N, O-( e. g., amino acidate), or O,O- ( e. g., beta-diketonate) chelating ligand, the arene ranges from benzene derivatives to fused polycyclic hydrocarbons, and Z is usually PF6. The X-ray structures of 13 complexes are reported. All have the characteristic "piano-stool" geometry. The complexes most active toward A2780 human ovarian cancer cells contained XY) ethylenediamine ( en) and extended polycyclic arenes. Complexes with polar substituents on the arene or XY) bipyridyl derivatives exhibited reduced activity. The activity of the O, O- chelated complexes depended strongly on the substituents and on the arene. For arene) p-cymene, XY) amino acidate complexes were inactive. Complexes were not cross-resistant with cisplatin, and cross-resistance to Adriamycin was circumvented by replacing XY) en with 1,2-phenylenediamine. Some complexes were also active against colon, pancreatic, and lung cancer cells.