Synthesis and biodistribution of novel (TcN)-Tc-99m complexes of glucose dithiocarbamate as potential probes for tumor imaging

In this study, two novel glucose dithiocarbamates (3a and 3b) were successfully synthesized via a "click chemistry" route and then radiolabeled with a [Tc-99m equivalent to N](2+) core to prepare the corresponding (TcN)-Tc-99m complexes in high yields. Both of them were hydrophilic and had good in vitro stability. The in vivo bio-distribution studies in mice bearing S180 tumor showed that the complexes accumulated in the tumor with high uptake and good retention. Through comparison, (TcN)-Tc-99m-3b had the advantages of higher tumor uptake, tumor/blood and tumor/muscle ratios at 2 h post-injection. The single-photon emission computed tomography (SPECT) image studies of (TcN)-Tc-99m-3b showed obvious radioactive uptake in the tumor region and the tumor-to-non-target ratio was high, suggesting that it could be regarded as a promising tumor imaging agent.National Natural Science Foundation of China [21171024, 21541001]SCI(E)ARTICLEzhjunbo@bnu.edu.cn; jinzhonghui@163.com71381-1386