Efficient synthesis of new phenanthridine Wnt/beta-catenin signaling pathway agonists
Chen, Duozhi1; Zhang, Heng2,3; Jing, Chenxu4; He, Xiaoli2; Yang, Bijuan1; Cai, Jieyun1; Zhou, Yunfu2; Song, Xiaoming2; Li, Lin2; Hao, Xiaojiang1
2018-09-05
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号157页码:1491-1499
摘要Previously, HLY78, a lycorine derivative, was identified as the first Wnt/beta-catenin signaling agonist through binding to the DAX domain of Axin, a scaffold of Wnt/beta-catenin complex. In this study, to obtain more potent Wnt/beta-catenin agonist, the structure optimization of HLY78 was carried out by design and synthesis of six phenanthridine derivatives, which afforded five active ones. In particular, 8,9-bis((1,3-dimethyl-1H-pyrazol)methoxy)-5-ethyl-4-methyl-5,6-dihydrophenanthridine showed the most potent activity (0.15/mu M) that was increased nearly 30 times as that of the lead HLY78. These compounds may be valuable in future pharmacological or biological studies. (C) 2018 Elsevier Masson SAS. All rights reserved.
关键词Wnt/beta-catenin signaling agonist Phenanthridine derivatives Structural optimization
资助信息National Natural Science Foundation of China; Central Asian Drug Discovery and Development Center of Chinese Academy of Sciences; Youth Innovation Promotion Association CAS; Yunnan Applied Basic Research Projects
语种英语
资助项目National Natural Science Foundation of China[81773610] ; National Natural Science Foundation of China[21432010] ; Central Asian Drug Discovery and Development Center of Chinese Academy of Sciences[CAM201702] ; Youth Innovation Promotion Association CAS[2018429] ; Yunnan Applied Basic Research Projects[2016FB015]
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文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/62781
专题植物化学与西部植物资源持续利用国家重点实验室
通讯作者Li, Lin; Hao, Xiaojiang
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol,Innovat Ctr Cell Signali, State Key Lab Mol Biol,CAS Ctr Excellence Mol Cel, Shanghai 200031, Peoples R China
3.Univ Chinese Acad Sci, Shanghai, Peoples R China
4.Changchun Univ Chinese Med, Affiliated Hosp, Res Ctr Tradit Chinese Med, Changchun 130021, Peoples R China
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Chen, Duozhi,Zhang, Heng,Jing, Chenxu,et al. Efficient synthesis of new phenanthridine Wnt/beta-catenin signaling pathway agonists[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,157:1491-1499.
APA Chen, Duozhi.,Zhang, Heng.,Jing, Chenxu.,He, Xiaoli.,Yang, Bijuan.,...&Hao, Xiaojiang.(2018).Efficient synthesis of new phenanthridine Wnt/beta-catenin signaling pathway agonists.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,157,1491-1499.
MLA Chen, Duozhi,et al."Efficient synthesis of new phenanthridine Wnt/beta-catenin signaling pathway agonists".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 157(2018):1491-1499.
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