Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents
Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents
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作为有效心血管药物的新型川芎嗪化衍生物的设计、合成和生物学评价
DOI：
10.1039/c3md20352b
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发表时间：
2013-04
期刊：
影响因子：
--
通讯作者：
Liu, Xinyong
中科院分区：
文献类型：
--
作者：
Chen, Hongfei;Li, Guoning;Zhan, Peng;Guo, Xiuli;Ding, Qian;Wang, Shouxun;Liu, Xinyong
设计、合成了一系列新型川芎嗪化衍生物，并评估了其对过氧化氢（H2O2）诱导的ECV-304细胞氧化损伤的保护作用，并测定了其对二磷酸腺苷（ADP）诱导的血小板聚集的抑制作用。生物学结果表明，一些化合物在一项或两项测定中表现出中等至有效的活性。在这些化合物中，化合物3对受损的ECV-304细胞显示出最高的保护作用，EC50 = 0.0040 mM，化合物1c是最活跃的血小板聚集抑制剂（EC50 = 0.40 mM）。简要讨论了结构-活性关系。
A series of novel ligustrazinylated derivatives was designed, synthesized and evaluated for their protective effects against hydrogen peroxide (H2O2)-induced oxidative damage on ECV-304 cells, and also assayed for their inhibition effects on platelet aggregation induced by adenosine diphosphate (ADP). Biological results showed that some compounds exhibited moderate to potent activities in one or both of the assays. Among these compounds, compound 3 displayed the highest protective effect on the damaged ECV-304 cells with EC50 = 0.0040 mM, and compound 1c was the most active platelet aggregation inhibitor (EC50 = 0.40 mM). Structure–activity relationships were briefly discussed.
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影响因子：
3.9
作者：
A. Palaniyappan;R. Alphonse
通讯作者：
A. Palaniyappan;R. Alphonse
影响因子：
3
作者：
Deng, Lijuan;Guo, Xiuli;Liu, Xinyong
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影响因子：
5
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影响因子：
2.7
作者：
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通讯作者：
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影响因子：
2.9
作者：
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通讯作者：
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