New Approaches to the Labeling of Estrogen Useful for PET.
Abstract
Positron Emission Tomography (PET) allows estrogen receptor-positive breast cancer to be diagnostically imaged using radiolabeled estrogens with the benefit of early detection, monitoring, and staging of breast cancer. In order to better target breast cancer, improved estrogen receptor imaging agents are sought. Three new estrogen receptor ligands were synthesized with a methoxy substituted at the 16 position. These compounds were obtained by utilizing the chemistry of methyl hypofluorite (MeOF). Conditions for reacting methyl hypofluorite and steroids were optimized overcoming solubility and solvent problems resulting in decreased formation of side products. Two of the three estradiol analogs were tested for their affinity to bind the estrogen receptor. The results predict these agents to be poor visualizers of breast tumors. The third estrogen, 16alpha-methoxyestradiol-17beta, is currently being tested and based on its structure is predicted to be the superior imaging agent of the three. Synthesis of this third compound required several modifications leaving it the last to be tested. If the binding affinity of this compound is found to be favorable, carbon-11 radiolabeling studies will be initiated to further evaluate the biological effectiveness.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jul 01, 1997
- Accession Number
- ADA344073
Entities
People
- Michael J. Welch
- Stephanie D. Johnson
Organizations
- Washington University in St. Louis