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

Abstract

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.