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This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of [Tc(CO)(PA-TZ-CHC)]. The novel colchicine (CHC) ligand was successfully synthesized via 'click' reaction. Radiolabeling was performed in high yield with [Tc(CO)] core to get [Tc(CO)(PA-TZ-CHC)], which was hydrophilic and cationic, and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [Tc(CO)(PA-TZ-CHC)] accumulated in the tumor with good uptake while comparatively low retention. The clearance of the 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. [ABSTRACT FROM AUTHOR]

This study reports the synthesis, radiolabeling and preliminary biodistribution results of [Tc(CO)(MN-TZ-BPA)] in tumor-bearing mice. The novel nitroimidazole derivative was successfully synthesized by conjugation of bis(pyridin-2-ylmethyl)amine (BPA) to 2-methyl-5-niroimidazole via 'click' reaction. The ligand could be labeled by [Tc(CO)] core in high yield to get [Tc(CO)(MN-TZ-BPA)], which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [Tc(CO)(MN-TZ-BPA)] accumulated in the tumor with certain initial uptake while poor retention. The rapid clearance from normal organs with favorable tumor/muscle ratios warrants further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled nitroimidazoles by structural modification. [ABSTRACT FROM AUTHOR]