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Synthesis and biological evaluation of novel 99m Tc‐oxo and 99m Tc‐tricarbonyl complexes with C3′‐functionalized thymidine dithiocarbamate for tumor imaging
Author(s) -
Duan Xiaojiang,
Gan Qianqian,
Song Xiaoqing,
Fang Si'an,
Zhang Xuran,
Ruan Qing,
Zhang Junbo
Publication year - 2018
Publication title -
applied organometallic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.53
H-Index - 71
eISSN - 1099-0739
pISSN - 0268-2605
DOI - 10.1002/aoc.4424
Subject(s) - chemistry , biodistribution , dithiocarbamate , rhenium , internalization , thymidine , nucleoside , radiochemistry , tumor cells , in vitro , stereochemistry , cancer research , cell , biochemistry , organic chemistry , biology
A novel C3′‐functionalized thymidine dithiocarbamate derivative (3’DTC‐TdR) was successfully synthesized and labelled using [ 99m TcO] 3+ core and [ 99m Tc(CO) 3 (H 2 O) 3 ] + core with high yields. The structures of the 99m Tc complexes were verified by preparation and characterization of the corresponding stable rhenium complexes. Both of the complexes were lipophilic and stable in vitro . Cell internalization experiments indicated that the uptakes of 99m TcO‐3’DTC‐TdR were related to nucleoside transporters. Biodistribution of these complexes in mice bearing tumor showed that they had high tumor uptakes, good tumor/muscle ratios and tumor/blood ratios. Especially for 99m TcO‐3’DTC‐TdR, it exhibited the highest tumor/muscle ratio and tumor/blood ratio at 4 h post‐injection. SPECT/CT imaging studies indicated clear accumulation in tumor, suggesting 99m TcO‐3’DTC‐TdR would be a promising candidate for tumor imaging.