Synthesis and Biological Evaluation of Caffeic Acid Amides as Selective Matrix Metalloproteinase Inhibitors

LI Nianguang; SHI Zhihao; SHI Qianping; TANG Hao; TANG Yuping

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Synthesis and Biological Evaluation of Caffeic Acid Amides as Selective Matrix Metalloproteinase Inhibitors

LI Nianguang 1 * #,SHI Zhihao 2,SHI Qianping 3,TANG Hao 4,TANG Yuping 1

1.Jiangsu Key Laboratory for High Technology of TCM Formulae, Nanjing University of Chinese Medicine, NanJing 210046

2. Department of Medicinal Chemistry, Nanjing University of Chinese Medicine, NanJing 210046

3.Department of Organic Chemistry, China Pharmaceutical University, NanJing 211198

4.Department of Medicinal Chemistry, Nanjing University of Chinese Medicine, NanJing 210046

*Correspondence author

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Funding: the Main Training Fund of Nanjing University of Chinese Medicine（No.10XPY02）, Research Fund for the Doctoral Program of Higher Education of China （No.20093237120012）

Opened online:17 September 2012

Accepted by: none

Citation: LI Nianguang,SHI Zhihao,SHI Qianping.Synthesis and Biological Evaluation of Caffeic Acid Amides as Selective Matrix Metalloproteinase Inhibitors[OL]. [17 September 2012] http://en.paper.edu.cn/en_releasepaper/content/4489061

A series of caffeic acid amides were synthesized, and through measurement using a fluorogenic substrate assay with human recombinant MMP-1, MMP-2 and MMP-9, compound 3f showed considerable inhibitory activities against MMP-2, MMP-9 and best selectivity over MMP-1. Prelimianay structure-activity relationship analysis indicated that caffeic acid amides with electron-donating groups at p-position of amino phenyl group showed better inhibitory activities and selectivity than those with electron-withdrawing groups. The findings of this study would provide information for the exploitation and utilization of caffeic acid as MMP inhibitor for metastatic tumour treatment.

Keywords:Caffeic acid; Metrix metalloproteinase; Tumour; Structure-activity relationship.

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