Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 24, Pages 8286-8294Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.09.015
Keywords
cinnamoyl pyrrolidine derivatives; MMPs inhibitors; IC50
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A series of new cinnamoyl pyrrolidine derivatives have been synthesized based on the L-hydroxyproline scaffold and inhibiting activities on gelatinase (MMP-2 and -9) and APN were tested. Structure-activity relationship studies showed that the side chain with aromatic ring at C4 in pyrrolidine ring showed better inhibitory activities on gelatinase than aliphatic side chain. Most compounds exhibited poor activities on APN compared with MMP-2. Within this series, three compounds, A8, B9 and C10, have the good potency (IC50 = 5.2-9.7 nM) and could be used as lead compounds in the future. (c) 2006 Elsevier Ltd. All rights reserved.
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