Synthesis, radiolabeling and biological distribution of a new dioxime derivative as a potential tumor imaging agent

摘要

A novel dioxime derivative (2E,2'E,3E,3'E)-3,3'-(pyrimidine-4,5-diylbis(azanylylidene))bis(butan-2-one)dioxime was synthesized with a yield of 65%. IR, elemental analysis, mass spectroscopy and H-1-NMR were used to characterize the structure of the synthesized compound. Tc-99m-dioxime was radio-synthesized with a high radiochemical yield of 97.8 +/- 0.5% and in vitro stability of 6 h under the optimum conditions. The preclinical evaluation of Tc-99m-dioxime in solid tumor-bearing mice showed high accumulation in solid tumor cells with a high Target/Non-Target ratio of 5.14 at 30 min post-injection. This study suggests that Tc-99m-dioxime derivative is a promising candidate as a new Tc-99m-based tumor-imaging agent after further preclinical studies.