Duan Xiaojiang, Liu Teli, Zhang Yichun, Zhang Junbo
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
Molecules. 2016 Apr 19;21(4):510. doi: 10.3390/molecules21040510.
Achieving a (99m)Tc labeled thymidine radiotracer for single photon emission tomography (SPECT) is considered to be of interest. In this study, four novel thymidine analogs, 6a, 6b, 6c and 6d, were successfully synthesized via "click reaction" route and then radiolabeled using a [(99m)Tc(CO)₃]⁺ core to prepare the corresponding (99m)Tc(CO)₃ complexes in high yields. These complexes were hydrophilic and had good in vitro stability. Biodistribution of these complexes in mice bearing S180 tumors showed that all of them exhibited accumulation in the tumors, suggesting that they would be potential tumor imaging agents.
获得用于单光子发射断层扫描（SPECT）的（99m）Tc标记的胸苷放射性示踪剂被认为是有意义的。在本研究中，通过“点击反应”路线成功合成了四种新型胸苷类似物6a、6b、6c和6d，然后使用[（99m）Tc（CO）₃]⁺核心进行放射性标记，以高产率制备相应的（99m）Tc（CO）₃配合物。这些配合物具有亲水性且在体外具有良好的稳定性。这些配合物在荷S180肿瘤小鼠体内的生物分布表明，它们在肿瘤中均有蓄积，提示它们可能是潜在的肿瘤显像剂。
