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
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume157Pages:1491-1499
AbstractPreviously, 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.
KeywordWnt/beta-catenin signaling agonist Phenanthridine derivatives Structural optimization
DOI10.1016/j.ejmech.2018.08.064
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000447480000104
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Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/62781
Collection植物化学与西部植物资源持续利用国家重点实验室
Corresponding AuthorLi, Lin; Hao, Xiaojiang
Affiliation1.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
Recommended Citation
GB/T 7714
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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