1. Synthesis, Tc(CO)-labeling and preliminary biodistribution studies of a novel colchicine complex.
- Author
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Wang, Jianjun, Duan, Xiaojiang, Mao, Huining, Yang, Jing, Tan, Cunmin, Tian, Yuan, and Wu, Wangsuo
- Subjects
TECHNETIUM isotopes ,CHEMICAL labeling ,COLCHICINE ,COMPLEX compounds synthesis ,RADIOLABELING ,LABORATORY mice ,CLICK chemistry - Abstract
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]
- Published
- 2013
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