Synthesis and preliminary biological evaluation of the 99mTc labeled nitrobenzoimidazole and nitrotriazole as tumor hypoxia markers

被引:39
作者
Zhang, Y
Chu, TW [1 ]
Gao, XG
Liu, XQ
Yang, Z
Guo, ZQ
Wang, XY
机构
[1] Peking Univ, Coll Chem & Mol Engn, Dept Appl Chem, Beijing 100871, Peoples R China
[2] Peking Univ, Sch Oncol, Beijing 100036, Peoples R China
[3] Beijing Inst Canc Res, Beijing 100036, Peoples R China
[4] Peking Univ, Coll Life Sci, Beijing 100871, Peoples R China
基金
中国国家自然科学基金;
关键词
hypoxia; nitrobenzoimidazole; nitrotriazole; tumor; labeling;
D O I
10.1016/j.bmcl.2006.01.001
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
1-(3-1 2,4-Nitrotriazole-1-yl)-propanhydroxyiminoamide and 1-(6-nitrobenzoimidazole-1-yl)-propanhydroxyiminoamide were synthesized and radiolabeled with Tc-99m. The Tc-99m labeled complexes continuously accumulated in hypoxic marine sarcoma S180 cells in vitro but not in aerobic cells. Biodistribution results in mice bearing S180 tumor indicated that the tracers could localize in tumor and eliminate from it slowly. These results suggested that the Tc-99m labeled nitrobenzoimidazole and nitrotriazole might be the novel tumor hypoxia markers. (C) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1831 / 1833
页数:3
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