Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists

doi:10.1021/acs.jnatprod.5b00825

	Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists
	Chen, Duo-Zhi 1; Jing, Chen-Xu 1; Cai, Jie-Yun 1; Wu, Ji-Bo 2; Wang, Sheng 2; Yin, Jun -Lin 1; Li, Xiao-Nian 1; Li, Lin 2; Hao, Xiao-Jiang1
	2016
发表期刊	JOURNAL OF NATURAL PRODUCTS
卷号	79 期号:1 页码:180-188
摘要	Lycorine 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.
DOI	10.1021/acs.jnatprod.5b00825
收录类别	SCI ; IC
语种	英语
WOS记录号	WOS:000368755000023
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/25949
专题	植物化学与西部植物资源持续利用国家重点实验室
作者单位	1.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
推荐引用方式 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.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
chen201135.pdf（3043KB）			开放获取	CC BY-NC-SA	浏览下载