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学科主题: 药学
题名:
Biological evaluation of novel selenazole-based compounds as potential thioredoxin reductase inhibitors
作者: Li, Dong-Dong1,2; He, Jie1; Zeng, Hui-Hui1,2
关键词: organoselenium compounds ; thioredoxin reductase inhibitors ; antitumor activity
刊名: APPLIED ORGANOMETALLIC CHEMISTRY
发表日期: 2012-11-01
DOI: 10.1002/aoc.2910
卷: 26, 期:11, 页:619-624
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Applied ; Chemistry, Inorganic & Nuclear
研究领域[WOS]: Chemistry
关键词[WOS]: CELL GROWTH-INHIBITION ; HUMAN CANCER-CELLS ; IN-VITRO ; ORGANOTELLURIUM COMPOUNDS ; ORGANOGOLD(III) COMPOUNDS ; RIBONUCLEOTIDE REDUCTASE ; GLUTATHIONE-REDUCTASE ; MOTEXAFIN GADOLINIUM ; GOLD COMPOUNDS ; APOPTOSIS
英文摘要:

Recently, thioredoxin reductase as a target for treatment of tumors has attracted the attention of scientists. 1,2-[Bis(1,2-benzisoselenazolone-3(2?H)-ketone)]ethane (ethaselen, BBSKE, PCT: CN02/00412), designed and synthesized previously, is an effective thioredoxin reductase inhibitor; presently it is in phase II clinical trials, targeting gastric cancer, lung cancer and colon cancer. To seek more novel and effective anticancer drugs, we have developed many selenazole-based compounds. Evaluation of the thioredoxin reductase inhibitory effect and investigation of the mechanism of anticancer drugs require abundant thioredoxin reductase, but since commercial thioredoxin reductase is expensive its use is often limited. Therefore, the preparation of thioredoxin reductase is necessary. Base on the above investigation, in this work we have prepared thioredoxin reductase and evaluated selenazole-based compounds, and found that 44 compounds have high inhibitory effect on thioredoxin reductase with IC50?

语种: 英语
所属项目编号: 2011 M500526
项目资助者: China Postdoctoral Science Foundation
WOS记录号: WOS:000310394300010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54074
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Tianjin Int Joint Acad Biotechnol & Med, Tianjin 300457, Peoples R China

Recommended Citation:
Li, Dong-Dong,He, Jie,Zeng, Hui-Hui. Biological evaluation of novel selenazole-based compounds as potential thioredoxin reductase inhibitors[J]. APPLIED ORGANOMETALLIC CHEMISTRY,2012,26(11):619-624.
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