Synthesis and structure–activity relationship analysis of caffeic acid amides as selective matrix metalloproteinase inhibitors
…, QP Shi, H Tang, YP Tang, W Li, L Yin, JP Yang…
Index: Shi, Zhi-Hao; Li, Nian-Guang; Shi, Qian-Ping; Tang, Hao; Tang, Yu-Ping; Li, Wei; Yin, Lian; Yang, Jian-Ping; Duan, Jin-Ao Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1206 - 1211
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Citation Number: 11
Abstract
Four series of 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 the best selectivity over MMP- 1. Preliminary structure–activity relationship analysis indicated that caffeic acid amides with electron-donating groups at para-position of amino phenyl group showed better inhibitory ...
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