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Synthesis and Biological Evaluation of Substituted Cinnamic Acid Esters as Selective MMP-2 and MMP-9 Inhibitors
LI Nianguang 1 * #,SHI Zhihao 2,TANG Hao 3,SHI Qianping 1,TANG Yuping 4
1.Jiangsu Key Laboratory for High Technology Reseach 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
#Submitted by
Subject:
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:23 July 2012
Accepted by: none
Citation: LI Nianguang,SHI Zhihao,TANG Hao.Synthesis and Biological Evaluation of Substituted Cinnamic Acid Esters as Selective MMP-2 and MMP-9 Inhibitors[OL]. [23 July 2012] http://en.paper.edu.cn/en_releasepaper/content/4484920
 
 
Substituted cinnamic acid esters with extended P1' group were synthesized under microwave irradiation and tested for their inhibitory activities on MMP-1, MMP-2 and MMP-9. Preliminary SARs analysis showed that hydroxyl groups in the benzene ring and the presence of extended spatial structures in the carboxylic acid played key roles in the MMP-2 and MMP-9 inhibitory activity and selectivity over MMP-1.
Keywords:matrix metalloproteinases; tumour; caffeic acid; structure-activity relationship
 
 
 

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