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 shu

Synthesis and preliminary biological evaluation of a technetium-99m labeled thymidine analog

a Key Laboratory of Nuclear Medicine, Ministry of Health/Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China;
b School of Chemical & Material Engineering, Jiangnan University, Wuxi 214122, China;
c Department of Food Science & Technology, School of Agriculture and Biology Shanghai Jiao Tong University, Shanghai 200240, China

Received Date: 2 April 2011

Fund Project: Financial support was provided by Natural Science Foundation of Jiangsu Province (no.BK2008112), and Department of Health of Jiangsu Province (no.H200624).

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.
- Synthesis,
- ^99mTc-NHT,
- Biodistribution,
- Thymidine analog,
- Tumor imaging
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