Δ3 - 2 - 羟基补骨脂酚类似物的合成及其对大鼠UMR106细胞的生长抑制活性
Synthesis of ∆3-2-hydroxybakuchiol analogues and their growth inhibitory activity against rat UMR106 cells.
作者信息
Zhao Qun, Xu Qianqian, Shan Guangsheng, Dong Chao, Zhang Hong, Lei Xinsheng
机构信息
School of Pharmacy, Fudan University, Shanghai 201203, China.
Department of Pharmaceutical Botany, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
出版信息
Molecules. 2014 Feb 20;19(2):2213-25. doi: 10.3390/molecules19022213.
A series of ∆3-2-hydroxybakuchiol analogues have been synthesized and tested for their growth inhibitory activity against rat UMR106 cells by using the MTT method. Some of them exhibit enhanced activities compared with the natural product, and the preliminary SAR profile shows that the chain tail on the natural product could be subtly modified to enhance the activity and the aromatic moiety or the terminal olefin on the main chain can also be modified without any evident loss of activity. The stereo-configuration of the quaternary chiral center has an important influence on the activity.
通过MTT法合成了一系列∆3 - 2 - 羟基补骨脂酚类似物，并测试了它们对大鼠UMR106细胞的生长抑制活性。其中一些与天然产物相比表现出增强的活性，初步的构效关系表明，天然产物上的链尾可以进行细微修饰以增强活性，主链上的芳香部分或末端烯烃也可以进行修饰而不会明显丧失活性。季碳手性中心的立体构型对活性有重要影响。
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