Synthesis and Biological Evaluation of Novel (99m)Tc(CO)₃-Labeled Thymidine Analogs as Potential Probes for Tumor Proliferation Imaging.
نویسندگان
چکیده
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.
منابع مشابه
Preparation and preliminary biological evaluation of novel (99m)Tc-labelled thymidine analogs as tumor imaging agents.
Two kinds of novel thymidine derivatives, N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-ethanediamine (TMHEA) and N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-hexanediamine (TMHHA) were prepared and successfully labeled with (99m)Tc in high labeling yields. The in vitro stability and in ...
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ورودعنوان ژورنال:
- Molecules
دوره 21 4 شماره
صفحات -
تاریخ انتشار 2016