Ligustrazine Derivatives. Part 4: Design, Synthesis, and Biological Evaluation of Novel Ligustrazine-based Stilbene Derivatives as Potential Cardiovascular Agents
Ligustrazine Derivatives. Part 4: Design, Synthesis, and Biological Evaluation of Novel Ligustrazine-based Stilbene Derivatives as Potential Cardiovascular Agents
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DOI：
10.1111/j.1747-0285.2012.01332.x
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发表时间：
2012-05-01
影响因子：
3
通讯作者：
Liu, Xinyong
中科院分区：
文献类型：
--
作者：
Deng, Lijuan;Guo, Xiuli;Liu, Xinyong
设计、合成了一系列含有川芎嗪基片段的新型苯乙烯衍生物，并测定了它们对受损内皮细胞的保护作用。结果表明，与川芎嗪相比，大多数川芎嗪基二苯乙烯衍生物对过氧化氢损伤的人脐血管内皮细胞（HUVECs）具有较高的保护作用。二苯乙烯衍生物A6、A9、A11、A21、A24、A25和A27效价较高，EC50值在0.0249 ~ 0.0898 mm范围内。化合物A27的EC50值为0.0249 μ m，比川芎嗪高出3万倍，具有较好的研究前景。简要讨论了构效关系。
A series of novel stilbene derivatives containing ligustrazinyl moiety was designed, synthesized, and assayed for their protective effects on damaged endothelial cells. The results showed that most ligustrazinyl stilbene derivatives exhibited high protective effects on the human umbilical vascular endothelial cells (HUVECs) damaged by hydrogen peroxide in comparison with Ligustrazine. The stilbene derivatives A6, A9, A11, A21, A24, A25, and A27 exhibited high potency with low EC50 values ranged from 0.0249 mu m to 0.0898 mm. Compound A27 displayed EC50 0.0249 mu m, which is 30 000 times higher than that of Ligustrazine, presenting a most promising lead for further investigation. Structureactivity relationships were briefly discussed.