Citation: Chun Xiong Lu, Zheng Wu Wang, Quan Fu Jiang, Jie Tang, Cheng Tan, Jian Kang Zhang. Synthesis and preliminary biological evaluation of a technetium-99m labeled thymidine analog[J]. Chinese Chemical Letters, ;2011, 22(11): 1309-1312. doi: 10.1016/j.cclet.2011.06.012
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The synthesis and labeling of 99mTc-N3-{N'-[2-sulfanyl-ethylamino)acetyl]-2-aminoethyl-sulfanyl-l-hexanamide}thymidine (99mTc-NHT) were studied. In the presence of sodium glucoheptonate (GH) and ethylene diamine tetraacetic acid (EDTA), 99mTc-NHT was obtained by using bisaminoethanethiol (N2S2) as a bifunctional coupling agent. The radiochemical purity of the 99mTc-NHT was over 95%. Biodistribution of 99mTc-NHT was performed in hepatoma HepA tumor-bearing mice. At 2 h p. i., the ratios of tumor-to-muscle, tumor-to-bone and tumor-to-blood were 4.41±0.32, 2.45±0.24 and 1.51±0.18, respectively.
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Keywords:
- Synthesis,
- 99mTc-NHT,
- Biodistribution,
- Thymidine analog,
- Tumor imaging
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