Book of Abstracts - Ruhr-Universität Bochum
Book of Abstracts - Ruhr-Universität Bochum
Book of Abstracts - Ruhr-Universität Bochum
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P-32<br />
ISBOMC `10 5.7 – 9.7. 2010 <strong>Ruhr</strong>-<strong>Universität</strong> <strong>Bochum</strong><br />
Organometallic Iridium Anticancer Complexes<br />
Zhe Liu, Abraha Habtemariam, Ana Pizarri, Sally Fletcher, Guy Clarkson and Peter J. Sadler<br />
Department <strong>of</strong> Chemistry, University <strong>of</strong> Warwick, Coventry CV4 7AL, U.K.<br />
E-mail: Z.Liu.2@warwick.ac.uk<br />
Cisplatin has been used to treat various types <strong>of</strong> cancers for over 30 years, however, a number <strong>of</strong><br />
serious side-effects <strong>of</strong> cisplatin have stimulated the long quest for other metal-based anticancer agents,<br />
especially drugs which possess a wider range <strong>of</strong> anticancer activity and with fewer side effects than<br />
cisplatin. There is much current interest in the design <strong>of</strong> ruthenium 1 and osmium 2 complexes as<br />
anticancer agents, but only a small amount <strong>of</strong> work has been done to investigate the antitumour<br />
activity <strong>of</strong> iridium complexes. 3<br />
Here we report the synthesis and characterization <strong>of</strong> a wide range <strong>of</strong> Ir(III) cyclopentadienyl<br />
complexes. We have studied their solid state structures, hydrolysis rates, reactivity towards<br />
nucleobases and acidity <strong>of</strong> aqua complexes. Their cell uptake and distribution and toxicity towards<br />
cancer cells have been studied and correlated with their chemical properties. Both the chemical and<br />
biological activity <strong>of</strong> these complexes show a strong dependence on the nature <strong>of</strong> the substituents on<br />
the cyclopentadienyl and the other ligands in the complexes.<br />
Acknowledgements: We thank WPRS (scholarship for Z.L), ERC (award for P.J.S.), EDRF and<br />
AWM for Science City funding, and members <strong>of</strong> COST Action D39 for stimulating discussions.<br />
References<br />
1. (a) A. Habtemariam, M. Melchart, R. Fernndez, S. Parsons, I. D. H. Oswald, A. Parkin, F. P. A.<br />
Fabbiani, J. E. Davidson, A. Dawson, R. E. Aird, D. I. Jodrell, P. J. Sadler, J. Med. Chem., 2006, 49,<br />
6858-6868. (b) J. M. Redemaker-Lakhai, D. van den. Bongard, D. Pluim, J. H. Beijnen, J. H. M.<br />
Schellens, Clin. Cancer Res. 2004, 10, 3717–3727. (c) I. Bratsos, S. Jedner, T. Gianferrara, E. Alessio,<br />
Chimia 2007, 61, 692-697.<br />
2. (a) A. F. A. Peacock, S. Parsons, P. J. Sadler, J. Am. Chem. Soc. 2007, 129, 3348-3357. (b) P.C. A.<br />
Bruijnincx and P. J. Sadler, Adv. Inorg. Chem. 2009, 61, 1-62.<br />
3. S. Schäfer, I. Ott, R. Gust, W. S. Sheldrick, Eur. J. Inorg. Chem. 2007, 3034-3046.<br />
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