Book of Abstracts - Ruhr-Universität Bochum

OP-35
ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum
Advances in Organometallic Chemistry for the Preparation of Molecular Imaging
and Therapy Agents
John F. Valliant*, a,b Anika Louie, a Alla Darwish, a Michael Cooke, a Antonio Toppino, a Karin
Stephenson, b Ryan Simms b
a McMaster University, Faculty of Science, Department of Chemistry, 1280 Main St. West, L8S 4M1,
Hamilton, Canada. b The Centre for Probe Development and Commercialization, McMaster
University, BSB-B231, 1280 Main St. West, L8S 4K1, Hamilton, Canada. E-mail:
valliant@mcmaster.ca
Medical isotopes that are metallic in nature are playing an increasingly important role in modern
nuclear medicine and basic biological research. 1 Delivering these radioisotopes to specific
biochemical targets while minimizing non-specific binding requires the development of new
prosthetic groups that form robust metal complexes in high yield under conditions that do not
degrade or modify sensitive targeting vectors. These prosthetic groups or ligands must also be
versatile with respect to how they are linked to targeting vectors and structurally modified in
order to meet the lipophilicity needs of the agent under development. With these requirements in
mind, organometallic complexes of Tc and Re are attractive platforms for developing new
imaging and therapy agents in that inert complexes can be formed in high yield using an array of
unique chelates and organometallic ligands. The work to be presented will include the
development of isostructural Re and Tc complexes that can be imaged in vitro and in vivo using
fluorescence microscopy and radioimaging methods respectively. 2 Complexes will include novel
chelates for the [M(CO)3] + core, which can be labeled at room temperature and incorporated into
peptide vectors as if they were natural amino acids. In addition, a new generation of isostructural
organometallic probes derived from carboranes will be presented. New labeling strategies for
tagging these molecules that go beyond conventional bulk solution methods will also be
discussed.
References
1. R. Alberto, J. Organomet. Chem. 2004, 692, 1179-1186.
2. K. Stephenson, S.R. Banerjee, T. Besanger, O.O. Sogbein, M.K. Levadala, N. McFarlane, J.
Lemon, D. R. Boreham, K. P. Maresca, J. D. Brennan, J. W. Babich, J. Zubieta, J. F. Valliant, J. Am.
Chem. Soc. 2004, 126, 8598-8599.
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