Synthesis, ~(99m)Tc(CO)_3-labeling and preliminary biodistribution studies of a novel colchicine complex

摘要

This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of [~(99m)Tc(CO) _3(PA-TZ-CHC)]~+. The novel colchicine (CHC) ligand was successfully synthesized via "click" reaction. Radiolabeling was performed in high yield with [~(99m)Tc(CO)_3]~+ core to get [~(99m)Tc(CO)_3(PA-TZ-CHC)]~+, which was hydrophilic and cationic, and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [~(99m)Tc(CO) _3(PA-TZ-CHC)]~+ accumulated in the tumor with good uptake while comparatively low retention. The clearance of the ~(99m)Tc-complex from normal organs was fast, resulting in increasing tumor/blood and tumor/muscle ratios. The promising results in preliminary biodistribution studies warrant further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled CHC derivative by structural modification.