Diagnostic and Therapeutic Radiopharmaceutical Agents for Selective Discrimination of Prostate Cancer; Annual rept. 1 Oct 2006-30 Sep 2007

摘要

The project investigated the development of ligand linked Flutamide analogs for complexing a M(CO)3 (Re,99mTc) organometallic species to target prostate cancer for imaging and therapy. The project has been successful in developing new synthetic strategies for this application. A general method was developed for preparing a universal flutamide analog that can be applied to number of ligands to yield a flutamide targeted species capable of delivery of M(CO)3 to the cancer cell. The chemical stability (heat, pH) was investigated and the application of this general coupling methodology was applied to several tridentate ligands(i.e., cysteine, histidine). The resulting flutamide linked ligand system were complexed with the M(CO)3 to yield the desired metal complex. The 99mTc complexes were prepared in excellent yields(>95%) at (10-4, 10-5 M) ligand concentration at biologically relevant pH and compared to the corresponding rhenium analogs through radio HPLC techniques.