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学科主题临床医学
Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents
Zhang, Chun Li1,2; Li, Tai Hua3; Niu, Shuang Huan3; Wang, Rong Fu2; Fu, Zhan Li2; Guo, Feng Qin2; Yang, Ming1
刊名BIOINORGANIC CHEMISTRY AND APPLICATIONS
2009
DOI10.1155/2009/908625
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Inorganic & Nuclear ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]ORGANIC GERMANIUM COMPOUND ; BIOLOGICAL-ACTIVITY ; GE-132 ; MICE ; CYTOTOXICITY ; CARCINOMA
英文摘要

Five new organogermanium sesquioxides have been synthesized and characterized by elemental analysis and IR spectra. All the compounds were tested for antitumor activities against KB, HCT, and Bel cells in vitro. Compound 5 (gamma-thiocarbamido propyl germanium sesquioxide) showed excellent antitumor activity, and its inhibition yield to KB, HCT, and Bel cells was 92.9%, 84.9%, and 70.9%, respectively. A rapid method was described for the labeling compound 5 with (99m)Tc, and the optimum labeling conditions were investigated. The labeling yield is above 90% in pH 7.0, 20 degrees C, reaction time greater than 10 minutes, 1 mg of compound 5, and 0.075 similar to 0.1 mg of SnCl(2). The biodistribution of (99m)Tc labeled compound 5 in nude mice bearing human colonic xenografts was studied. The result showed that the tumor uptakes were 0.73, 0.97, 0.87, and 0.62 ID%/g at 1-hour, 3-hour, 6-hour, and 20-hour postinjection, respectively. T/NT (the uptake ratio for per gram of tumor over normal tissues) was 18.3 for tumor versus brain and 5.81 for tumor versus muscle at 20-hour postinjection. The tumor clearance was slow. The results showed that compound 5 may be developed to be a suitable cancer therapeutic agent. Copyright (C) 2009 Chun Li Zhang et al.

语种英语
WOS记录号WOS:000267452900001
引用统计
被引频次:11[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/400002259/58057
专题北京大学第一临床医学院_核医学科
作者单位1.Peking Univ, Hlth Sci Ctr, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
2.Peking Univ, Hosp 1, Dept Nucl Med, Beijing 100034, Peoples R China
3.Beijing Normal Univ, Dept Chem, Beijing 100875, Peoples R China
推荐引用方式
GB/T 7714
Zhang, Chun Li,Li, Tai Hua,Niu, Shuang Huan,et al. Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents[J]. BIOINORGANIC CHEMISTRY AND APPLICATIONS,2009.
APA Zhang, Chun Li.,Li, Tai Hua.,Niu, Shuang Huan.,Wang, Rong Fu.,Fu, Zhan Li.,...&Yang, Ming.(2009).Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents.BIOINORGANIC CHEMISTRY AND APPLICATIONS.
MLA Zhang, Chun Li,et al."Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents".BIOINORGANIC CHEMISTRY AND APPLICATIONS (2009).
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