Synthesis and in vitro evaluation of three 99mTc-labeled hydroxamamide-based ligands as markers for hypoxic cells

被引：7
|
作者：
Chu, Taiwei [1 ]
Xu, Hong [1 ]
Yang, Zhi [2 ,3 ]
Wang, Xiangyun [1 ]
机构：
[1] Peking Univ, BNLMS, Dept Appl Chem, Coll Chem & Mol Engn, Beijing 100871, Peoples R China
[2] Peking Univ, Sch Oncol, Beijing 100036, Peoples R China
[3] Peking Univ, Beijing Inst Canc Res, Beijing 100036, Peoples R China
来源：
APPLIED RADIATION AND ISOTOPES | 2009年 / 67卷 / 04期
基金：
北京市自然科学基金; 中国国家自然科学基金;
关键词：
(99m)Tc complex; Hypoxia marker; Lipophilicity; Hydroxamamide; Labeling; TUMOR HYPOXIA; TC-99M RADIOPHARMACEUTICALS; TETRADENTATE LIGANDS;
D O I：
10.1016/j.apradiso.2008.12.003
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
Three new hydroxamamide derivatives with different lipophilicity, N'-hydroxy-N-methyl-3-(4-nitro-1H-imidazol-1-yl)propanamidine, N-butyl-N'-hydroxy-3-(4-nitro-1H-imidazol-1-yl)propanamidine, and N'-hydroxy-3-(4-nitro-1H-imidazol-1-yl)-N-octadecyl propanamidine were easily synthesized and labeled with technetium-99m as markers for hypoxic cells. The results of in vitro experiment indicate that the accumulation of three (99m)Tc-complexes steadily increases with time in hypoxic cells, but fluctuates with time and has no fixed trend in aerobic cells; the complex with higher lipophilicity shows more uptake in cells; and the effect of lipophilicity of the (99m)Tc-complexes on the hypoxic/aerobic difference can be neglected. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：590 / 593
页数：4
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