Ligustrazine Derivatives. Part 4: Design, Synthesis, and Biological Evaluation of Novel Ligustrazine-based Stilbene Derivatives as Potential Cardiovascular Agents

被引：23

作者：

Deng, Lijuan ^{[1
,2
]}

Guo, Xiuli ^{[1
]}

Zhai, Li ^{[1
]}

Song, Yuning ^{[1
]}

Chen, Hongfei ^{[1
]}

Zhan, Peng ^{[1
]}

Wu, Jingde ^{[1
]}

Liu, Xinyong ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Jinan 250012, Peoples R China

[2] Pingxiang Peoples Hosp, Medicament Dept, Pingxiang 337000, Peoples R China

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2012年 / 79卷 / 05期

关键词：

cardiovascular activity; ligustrazine; stilbene derivatives; synthesis; HYDROGEN-PEROXIDE; NA+/H+ EXCHANGER; TETRAMETHYLPYRAZINE; INHIBITORS; AMILORIDE; INJURY; RATS;

D O I：

10.1111/j.1747-0285.2012.01332.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：731 / 739

页数：9

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