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Issue 5, 2013
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Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents

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Abstract

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.

Graphical abstract: Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents

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Publication details

The article was received on 22 Nov 2012, accepted on 10 Mar 2013 and first published on 11 Mar 2013


Article type: Concise Article
DOI: 10.1039/C3MD20352B
Citation: Med. Chem. Commun., 2013,4, 827-832

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    Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents

    H. Chen, G. Li, P. Zhan, X. Guo, Q. Ding, S. Wang and X. Liu, Med. Chem. Commun., 2013, 4, 827
    DOI: 10.1039/C3MD20352B

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