New Approaches to the Labeling of Estrogens Useful for PET (Predoctoral Training Program)

摘要

By incorporating a positron-emitting radionuclide into an estrogen receptor ligand, estrogen receptor-positive breast cancer can be visualized with Positron Emission Tomography (PET). In the search for improved estrogen receptor imaging agents, three isomers of 16-methoxyestradiol were synthesized via two synthetic routes, each utilizing methyl hypofluorite. The unusual chemistry of methyl hypofluorite provides a previously unexplored route for functionalizing the 16-position of estradiol and would provide a means of rapidly incorporating carbon-11 into biomolecules. The estrogen receptor binding affinities for these isomers determined these compounds to be ineffective imaging agents for the estrogen receptor.