期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 18, 页码 5638-5641出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.124
关键词
Lipogenic inhibitors; Boron-containing stilbene derivatives; Sterol regulatory element binding proteins (SREBPs); Wittig reaction; Lipid-lowering drugs
资金
- AECOM
- DRTC [P60 DK020541]
A pilot library of novel 4,4,5,5-tetramethyl-2-(4-substitutedstyrylphenyl)-1,3,2 dioxaborolane derivatives has been synthesized. 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaboratophenyl)-methyl triphenylphosphonium bromide 3 was treated with various aldehydes in the presence of 3 equiv of (BuONa)-Bu-t in DMF, and stirred at room temperature for 4-6 h to yield the corresponding boron-containing stilbene derivatives in 71-94% yields. Several of them, including BF102 and BF175, have the lipogenesis inhibitory effect by suppressing lipogenic gene expression in mammalian hepatocytes. Further, BF102 also inhibits cholesterol biosynthesis by suppressing HMG-CoA reductase gene expression in hepatocytes. Interestingly, our preliminary in vivo data suggests that BF102 has no significant toxicity in mice at the highest possible dose we can administered. Thus, BF102 is a potential lead for the next generation of lipid-lowering drugs. (C) 2011 Elsevier Ltd. All rights reserved.
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