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

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

机构地区：[1]Key Laboratory of Nuclear Medicine, Ministry of Health/Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China [2]School of Chemical ＆ Material Engineering, Jiangnan University, Wuxi 214122, China [3]Department of Food Science ＆ Technology, School of Agriculture and Biology Shanghai Jiao Tong University, Shanghai 200240, China

出　　处：《Chinese Chemical Letters》2011年第11期1309-1312,共4页中国化学快报（英文版）

基　　金：provided by Natural Science Foundation of Jiangsu Province(NoBK2008112);Department of Health of Jiangsu Province(NoH200624)

摘　　要：The synthesis and labeling of ^（99m）Tc-N^3-（N＇-[2-sulfanyl-ethylamino）acetyl]-2-aminoethyl-sulfanyl-1-hexanamide}thymidine （^（99m）Tc-NHT） were studied.In the presence of sodium glucoheptonate（GH） and ethylene diamine tetraacetic acid（EDTA）,^（99m）Tc-NHT was obtained by using bisaminoethanethiol（N_2S_2） as a bifunctional coupling agent.The radiochemical purity of the ^（99m）Tc-NHT was over 95%.Biodistribution of ^（99m）Tc-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.The synthesis and labeling of ^（99m）Tc-N^3-（N＇-[2-sulfanyl-ethylamino）acetyl]-2-aminoethyl-sulfanyl-1-hexanamide}thymidine （^（99m）Tc-NHT） were studied.In the presence of sodium glucoheptonate（GH） and ethylene diamine tetraacetic acid（EDTA）,^（99m）Tc-NHT was obtained by using bisaminoethanethiol（N_2S_2） as a bifunctional coupling agent.The radiochemical purity of the ^（99m）Tc-NHT was over 95%.Biodistribution of ^（99m）Tc-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.

关 键 词：SYNTHESIS ^（99m）Tc-NHT BIODISTRIBUTION Thymidine analog Tumor imaging 

分 类 号：TQ457.2[化学工程—农药化工] X826[环境科学与工程—环境工程]