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

Chun Xiong Lu Zheng Wu Wang Quan Fu Jiang Jie Tang Cheng Tan Jian Kang Zhang

引用本文: 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
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

  • 基金项目:

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

摘要: 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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  • 收稿日期:  2011-04-02
通讯作者: 陈斌, bchen63@163.com
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