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Biological evaluation of novel selenazole-based compounds as potential thioredoxin reductase inhibitors
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
2012-11-01
DOI10.1002/aoc.2910
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
WOS记录号WOS:000310394300010
引用统计
被引频次:5[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/400002259/54074
专题北京大学药学院
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
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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.
APA Li, Dong-Dong,He, Jie,&Zeng, Hui-Hui.(2012).Biological evaluation of novel selenazole-based compounds as potential thioredoxin reductase inhibitors.APPLIED ORGANOMETALLIC CHEMISTRY,26(11),619-624.
MLA Li, Dong-Dong,et al."Biological evaluation of novel selenazole-based compounds as potential thioredoxin reductase inhibitors".APPLIED ORGANOMETALLIC CHEMISTRY 26.11(2012):619-624.
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