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学科主题: 临床医学
题名:
Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents
作者: 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
发表日期: 2009
DOI: 10.1155/2009/908625
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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/58057
Appears in Collections:北京大学第一临床医学院_核医学科_期刊论文

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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

Recommended Citation:
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.
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