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Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK

文献类型：期刊论文

作者Shen, Sida2; Zhuang, Jingjing2; Chen, Yijia1; Lei, Min1; Chen, Jing1,3; Shen, Xu1,2; Hu, Lihong1,2
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2013-07-01
卷号21期号:13页码:3882-3893
关键词Arctigenin 9-Deoxy-arctigenin AMPK 2-(3,4-Dimethoxyphenyl)ethyl
ISSN号0968-0896
DOI10.1016/j.bmc.2013.04.010
文献子类Article
英文摘要A series of new arctigenin and 9-deoxy-arctigenin derivatives bearing different ester and ether side chains at the phenolic hydroxyl positions are designed, synthesized, and evaluated for activating AMPK potency in L6 myoblasts. Initial biological evaluation indicates that some alkyl ester and phenethyl ether arctigenin derivatives display potential activities in AMPK phosphorylation improvement. Further structure-activity relationship analysis shows that arctigenin ester derivatives 3a, 3h and 9-deoxy-arctigenin phenethyl ether derivatives 6a, 6c, 6d activate AMPK more potently than arctigenin. Moreover, the 2-(3,4-dimethoxyphenyl)ethyl ether moiety of 6c has been demonstrated as a potential functional group to improve the effect of AMPK phosphorylation. The structural optimization of arctigenin leads to the identification of 6c as a promising lead compound that exhibits excellent activity in AMPK activation. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.
WOS关键词PROTEIN-KINASE ; METABOLIC SYNDROME ; CANCER-CELLS ; (-)-ARCTIGENIN ; INHIBITION ; PATHWAY
资助项目National Natural Science Foundation of China[30925040] ; National Natural Science Foundation of China[81102329] ; National Natural Science Foundation of China[81273430] ; Chinese National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2013ZX09508104] ; Chinese National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2012ZX09301001-001] ; Chinese National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2011ZX09307-002-03] ; Science Foundation of Shanghai[12XD14057] ; State Key Laboratory of Natural and Biomimetic Drugs[K20120220]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000320347100027
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/277560]  
专题药理学第三研究室
通讯作者Shen, Xu
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China;
2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China;
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714		 Shen, Sida,Zhuang, Jingjing,Chen, Yijia,et al. Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2013,21(13):3882-3893.
APA Shen, Sida.,Zhuang, Jingjing.,Chen, Yijia.,Lei, Min.,Chen, Jing.,...&Hu, Lihong.(2013).Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK.BIOORGANIC & MEDICINAL CHEMISTRY,21(13),3882-3893.
MLA Shen, Sida,et al."Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK".BIOORGANIC & MEDICINAL CHEMISTRY 21.13(2013):3882-3893.

入库方式： OAI收割

来源：上海药物研究所

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