Phosphoramidate-based Peptidomimetic Prostate Cancer PET Imaging Agents.

摘要

The main goal is to develop a PET imaging agent based on modifying the peptidomimetic PSMA inhibitor which will result in improved tumor uptake and clearance mechanism. Different fluorination approaches were attempted with PSMA module compounds such as direct labeling, cupper free chemistry and the use of prosthetic group (SFB). The direct labeling approach has been eliminated as an option due to the instability of the fluorination. As for the cupper free chemistry labeling approach, the final purification step is in progress to provide a final product with higher specific activity (less mass for better imaging). In addition, the production of SFB has been attempted for labeling the module compounds as well and the work is ongoing. Once the labeling approaches are established, and then the labeling of the modified PSMA inhibitor analogues will be investigated in vitro as well as in vivo.