Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists
Chen, Duo-Zhi1; Jing, Chen-Xu1; Cai, Jie-Yun1; Wu, Ji-Bo2; Wang, Sheng2; Yin, Jun -Lin1; Li, Xiao-Nian1; Li, Lin2; Hao, Xiao-Jiang1
2016
Source PublicationJOURNAL OF NATURAL PRODUCTS
Volume79Issue:1Pages:180-188
AbstractLycorine is a benzylphenethylamine-type alkaloid member of the Amaryllidaceae family. A lycorine derivative, HLY78, was previously identified as a new Wnt/beta-catenin signaling pathway agonist that targets the DAX domain of axin. Herein, the structural optimization of HLY78 and analyses of the structure-activity relationships of lycorine-derived phenanthridine derivatives as agonists of the Wnt/beta-catenin signaling pathway are presented. This research suggests that triazole groups are important pharmacophores for Wnt activation; triazole groups at C-8 and C-9 of phenanthridine compounds markedly enhanced Wnt activation. A C-11-C-12 single bond is also important for Wnt activation. On the basis of these findings, two Wnt agonists were designed and synthesized. The results for these agonists indicated that the combination of a 4-ethyldihydrophenanthridine skeleton and a triazole substituent improves Wnt activation. These compounds may be useful in further pharmacological or biological studies.
DOI10.1021/acs.jnatprod.5b00825
Indexed BySCI ; IC
Language英语
WOS Research AreaPlant Sciences ; Pharmacology & Pharmacy
WOS SubjectPlant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy
WOS IDWOS:000368755000023
Citation statistics
Cited Times:10[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/25949
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, State Key Lab Mol Biol, Shanghai 200000, Peoples R China
Recommended Citation
GB/T 7714
Chen, Duo-Zhi,Jing, Chen-Xu,Cai, Jie-Yun,et al. Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists[J]. JOURNAL OF NATURAL PRODUCTS,2016,79(1):180-188.
APA Chen, Duo-Zhi.,Jing, Chen-Xu.,Cai, Jie-Yun.,Wu, Ji-Bo.,Wang, Sheng.,...&Hao, Xiao-Jiang.(2016).Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists.JOURNAL OF NATURAL PRODUCTS,79(1),180-188.
MLA Chen, Duo-Zhi,et al."Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists".JOURNAL OF NATURAL PRODUCTS 79.1(2016):180-188.
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