Synthesis and Biological Evaluation of Novel (99m)Tc(CO)₃-Labeled Thymidine Analogs as Potential Probes for Tumor Proliferation Imaging.
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.
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China. duanxj10@gmail.com.
Xiaojiang
X
Duan
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China. liuteli123321@163.com.
Teli
T
Liu
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China. zhangyichunkeke@163.com.
Yichun
Y
Zhang
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China. zhjunbo@bnu.edu.cn.
Junbo
J
Zhang
D000818:Animals; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D057930:Click Chemistry; D004355:Drug Stability; D051379:Mice; D009368:Neoplasm Transplantation; D015609:Organotechnetium Compounds / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D012509:Sarcoma / Q000000981:diagnostic imaging*; D013936:Thymidine / Q000031:analogs & derivatives*
D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D013936:Thymidine
[99mTc(CO)3]+ core; click chemistry; macrocyclic triamine; thymidine analogs; tumor proliferation imaging