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学科主题: 药学
题名:
Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy
作者: He, Jie1,2; Li, Dongdong3; Xiong, Kun1,2; Ge, Yongjie1,2; Jin, Hongwei1; Zhang, Guozhou1,2; Hong, Mengshi1,2; Tian, Yongliang1,2; Yin, Jin1,2; Zeng, Huihui1,2,3
关键词: Organoselenium compound ; Thioredoxin reductase ; Anticancer drug ; Structure-activity relationship
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2012-06-15
DOI: 10.1016/j.bmc.2012.04.033
卷: 20, 期:12, 页:3816-3827
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: CELL LUNG-CANCER ; MOTEXAFIN GADOLINIUM ; GROWTH-INHIBITION ; IN-VITRO ; MECHANISM ; SELENOCYSTEINE ; CARCINOMA ; ETHASELEN ; RADIOTHERAPY ; PROGRESSION
英文摘要:

Thioredoxin reductase (TrxR) is critical for cellular redox regulation and is involved in tumor proliferation, apoptosis and metastasis. Its C-terminal redox-active center contains a cysteine (Cys497) and a unique selenocysteine (Sec498), which are exposed to solvent and easily accessible. Thus, it is becoming an important target for anticancer drugs. Selective inhibition of TrxR by 1,2-(bis-1,2-benzisoselenazol-3(2H)-one)ethane (4a) prevents proliferation of several cancer cell lines both in vivo and in vitro. Using the structure of 4a as a starting point, a series of novel bis-1,2-benzisoselenazol-3(2H)-ones was designed, prepared and tested to explore the structure-activity relationships (SARs) for this class of inhibitor and to improve their potency. Notably, 1,2-(5,5′-dimethoxybis(1,2-benzisoselenazol-3(2H)-one))ethane (12) was found to be more potent than 4a in both in vitro and in vivo evaluation. Its binding sites were confirmed by biotin-conjugated iodoacetamide assay and a SAR model was generated to guide further structural modification. (C) 2012 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 2011M500526
项目资助者: China Postdoctoral Science Foundation
WOS记录号: WOS:000304486500015
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60938
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, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
3.Tianjin Int Joint Acad Biotechnol & Med, Tianjin 300457, Peoples R China

Recommended Citation:
He, Jie,Li, Dongdong,Xiong, Kun,et al. Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2012,20(12):3816-3827.
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