Synthesis and biological studies of ^99mTc(HYNIC-MFL)(tricine)(TPPTS) as a novel tumor imaging agent

This work reports the synthesis, radiolabeling and biological studies of ^99mTc(HYNIC-MFL)(tricine)(TPPTS) in tumor-bearing mice. The novel melphalan derivative was successfully synthesized by conjugation of HYNIC to melphalan. The ligand could be labeled by ^99mTc in high yield to get ^99mTc(HYNIC-MFL)(tricine)(TPPTS), which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that ^99mTc(HYNIC-MFL)(tricine)(TPPTS) accumulated in the tumor with favorable uptake and retention. The good accumulation in tumor tissue, high tumor/muscle ratios and satisfactory scintigraphic images highlight the potential of ^99mTc(HYNIC-MFL)(tricine)(TPPTS) for tumor imaging. (author)