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Design, Synthesis and Biological Evaluation of Ferulic Acid Amides as Selective Matrix Metalloproteinase Inhibitors

[ Vol. 9 , Issue. 7 ]

Author(s):

Zhi-Hao Shi, Nian-Guang Li, Qian-Ping Shi, Hao-Tang, Yu-Ping Tang, Wei-Li, Lian-Yin, Jian-Ping Yang and Jin-Ao Duan   Pages 947 - 954 ( 8 )

Abstract:


A series of ferulic acid amides with extended P1' groups were synthesized and tested for their inhibitory activities on matrix metalloproteinase (MMP)-1, MMP-2, and MMP-9. Preliminary structure–activity relationship analysis and docking studies indicated that ferulic acid amides with electron-donating groups at the amino phenyl ring showed better inhibitory activities and selectivity than those with electron-withdrawing groups. Compound 3e, which had a hydroxyl group at meta-position of amino phenyl ring, showed considerable inhibitory activities against MMP-2, MMP-9 and best selectivity over MMP-1. The findings of this study would provide information for the exploitation and utilization of ferulic acid as MMP inhibitor for metastatic tumor treatment.

Keywords:

Design, ferulic acid, inhibitor, metrix metalloproteinase, structure-activity relationship, tumor.

Affiliation:

Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, 138 Xianlin Road, 210046, Nanjing, Jiangsu, People’s Republic of China.



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