Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 15, Pages 4558-4560Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.06.021
Keywords
beta-Secretase; BACE-1; Alzheimer; Amentoflavone; Biflavonoid; 2,3-Dihydroamentoflavone; 2,3-Dihydro-6-methylginkgetin
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Funding
- Japan Society for the Promotion of Science (JSPS)
- High-Tech Research Center, Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan [S0801043]
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Here, we describe amentoflavone-type biflavonoids, which were isolated from natural sources and were found to inhibit beta-secretase (BACE-1). The structure-activity relationship was studied, and compounds 1-8, 10, 17, and 18 showed BACE-1 inhibitory activity. Among these compounds, 2,3-dihydroamentoflavone 17 and 2,3-dihydro-6-methylginkgetin 18 exhibited potent inhibitory effects with IC(50) values of 0.75 and 0.35 mu M, respectively. (C) 2010 Elsevier Ltd. All rights reserved.
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