Kinetically-inert organometallic ruthenium arene complexes: A new class of cancer cell cytotoxic agents

INOR 147

Sarah J Dougan, s.j.dougan-1@sms.ed.ac.uk1, Arindam Mukherjee2, Abraha Habtemariam2, and Peter J Sadler2. (1) Department of Chemistry, The University of Edinburgh, Kings Buildings, West Mains Road, EH9 3JJ Edinburgh, United Kingdom, (2) Department of Chemistry, The University of Warwick, Gibbet Hill Road, CV4 7AL, Coventry, United Kingdom
We are investigating the design of half-sandwich phenylazopyridine (azpy) complexes of the type [(η 6-arene)Ru(azpy)X]n+ as cancer cell cytotoxic agents (1). Remarkably we find that certain choices of azpy derivative and monodentate ligand X give rise to complexes which are inert to aquation and yet exhibit high activity towards both ovarian and lung cancer cells (IC50 1-6 µM). Our studies suggest that these complexes are activated in cells by reduction of the azpy ligand with subsequent generation of reactive oxygen species which damage the cells. (1) Dougan, S.J.; Melchart, M.; Habtemariam, A.; Parsons, S.; Sadler, P.J. Inorg. Chem. 2006, 45, 10882-10894.
 

Bioinorganic Chemistry: DNA and RNA
1:30 PM-5:30 PM, Sunday, August 19, 2007 BCEC -- 211, Oral

Division of Inorganic Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007