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Synthesis and biodistribution of novel Tc-99m labeled 4-nitroimidazole dithiocarbamate complexes as potential agents to target tumor hypoxia
Li, Zhenxiang1; Zhang, Junbo1; Jin, Zhonghui2; Zhang, Weifang2; Zhang, Yanyan2
刊名MEDCHEMCOMM
2015
DOI10.1039/c5md00042d
6期:6页:1143-1148
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
关键词[WOS]BIOLOGICAL EVALUATION ; DEOXYGLUCOSE DITHIOCARBAMATE ; MARKERS
英文摘要

Sodium 3-(4-nitro-1H-imidazolyl) propyl dithiocarbamate (N4IPDTC) was synthesized and radiolabelled with a [(99)mTcO](3+), [(99)mTc N](2+) or [(99)mTc(CO)(3)](+) core to produce (99)mTcO-N4IPDTC, (99)mTcN-N4IPDTC and (99)mTc(CO)(3)-N4IPDTC, respectively. All of the three complexes were prepared with high radiochemical purity and had good in vitro stability over a period of 6 h. The partition coefficient results showed that (99)mTcO-N4IPDTC and (99)mTcN-N4IPDTC were lipophilic, while (99)mTc(CO)(3)-N4IPDTC was hydrophilic. The tumor cell experiments and the biodistribution in mice bearing S180 tumors showed that all of the complexes exhibited good hypoxic selectivity and accumulation in the tumor. Among them, (99)mTcO-N4IPDTC had the advantages of higher tumor uptake, and higher tumor/blood and tumor/muscle ratios. Planar scintigraphic imaging studies showed there was a visible accumulation in tumor sites, suggesting its potential usefulness as a tumor hypoxia imaging agent.

语种英语
WOS记录号WOS:000355985500018
项目编号21171024 ; 81101069 ; 7112035
资助机构National Natural Science Foundation of China ; Beijing Natural Science Foundation
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/57861
专题北京大学第三临床医学院_核医学科
作者单位1.Beijing Normal Univ, Minist Educ, Coll Chem, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
2.Peking Univ, Hosp 3, Dept Nucl Med, Beijing 100191, Peoples R China
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GB/T 7714
Li, Zhenxiang,Zhang, Junbo,Jin, Zhonghui,et al. Synthesis and biodistribution of novel Tc-99m labeled 4-nitroimidazole dithiocarbamate complexes as potential agents to target tumor hypoxia[J]. MEDCHEMCOMM,2015,6(6):1143-1148.
APA Li, Zhenxiang,Zhang, Junbo,Jin, Zhonghui,Zhang, Weifang,&Zhang, Yanyan.(2015).Synthesis and biodistribution of novel Tc-99m labeled 4-nitroimidazole dithiocarbamate complexes as potential agents to target tumor hypoxia.MEDCHEMCOMM,6(6),1143-1148.
MLA Li, Zhenxiang,et al."Synthesis and biodistribution of novel Tc-99m labeled 4-nitroimidazole dithiocarbamate complexes as potential agents to target tumor hypoxia".MEDCHEMCOMM 6.6(2015):1143-1148.
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