Design, Synthesis, and Structural Optimization of Lycorine-Derived Phenanthridine Derivatives as Wnt/beta-Catenin Signaling Pathway Agonists
文献类型：期刊论文
| 作者 | 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
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| 刊名 | JOURNAL OF NATURAL PRODUCTS
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| 出版日期 | 2016 |
| 卷号 | 79期号:1页码:180-188 |
| 英文摘要 | 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. |
| 类目[WOS] | Plant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy |
| 研究领域[WOS] | Plant Sciences ; Pharmacology & Pharmacy |
| 关键词[WOS] | CANCER ; HSC70 ; CELLS |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000368755000023 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/25949]  |
| 专题 | 昆明植物研究所_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. |
入库方式： OAI收割
来源：昆明植物研究所
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