Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 2, Pages 548-552Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.11.073
Keywords
Positron emission tomography; Copper-64; Side-bridged cyclam; Bifunctional chelating agent
Funding
- NIH
- National Cancer Institute
- Center for Cancer Research
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Copper-64 (t(1/2) = 12.7 h; beta(+): 0.653 MeV, 17.4%; beta: 0.578 MeV, 39%) is produced in a biomedical cyclotron and has applications in both imaging and therapy. Macrocyclic chelators are widely used as bifunctional chelators to bind copper radionuclides to antibodies and peptides owing to their relatively high kinetic stability. A novel side-bridged cyclam featuring both pendant acetate and phosphonate groups was synthesized using a Kabachnik-Fields approach followed by hydrobromic acid deprotection. The Cu(II) complex of the novel ligand was synthesized, radiolabeling with Cu-64 was demonstrated, and in vitro (serum) stability was performed. In addition, in vivo distribution and clearance of the Cu-64-labeled complex was visualized by positron emission tomography (PET) imaging. This novel chelate may be useful in Cu-64-mediated diagnostic positron emission tomography (PET) imaging as well as targeted radiotherapeutic applications. Published by Elsevier Ltd.
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