Diagnostic and Therapeutic Radiopharmaceutical Agents for Selective Discrimination of Prostate Cancer

摘要

The project investigated the development of ligand linked Flutamide analogs for complexing M(CO)3 (Re,99mTc) organometallic species to target prostate cancer. The project has been successful in developing and testing new synthetic strategies for this application. General methods were established for preparing the cold Re and 99mTc complexes in excellent yields(>95%) at (10-4,10- 5 M) ligand concentration, testing the stability of the complexes (pH, temperature) and in vitro (serum, AR +/- prostate cancer cells). Several 99mTc flutamide analogs were examined. Tridentate ligands (i.e., cysteine, histidine, dipyridylamine, iminodiacetic acid) were successfully prepared and maintained stability in vitro. The '2+1' approach analogs were prepared, however, failed to maintain the complex conformation, when examined under biological conditions. Second generation compounds based on the initial experiments with addition functional group are currently being investigated.