Synthesis and inhibitory activity against COX-2 catalyzed prostaglandin production of chrysin derivatives
Synthesis and inhibitory activity against COX-2 catalyzed prostaglandin production of chrysin derivatives
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DOI：
10.1016/j.bmcl.2003.12.087
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发表时间：
2004-03-08
影响因子：
2.7
通讯作者：
Park, H
中科院分区：
文献类型：
--
作者：
Dao, TT;Chi, YS;Park, H
合成了一系列白杨素衍生物，并评价了它们对环氧合酶-2催化的前列腺素合成的抑制活性。以2-羟基苯乙酮、2，4-二羟基苯乙酮和2，6-二羟基苯乙酮为原料，经2~4步反应制得白杨素衍生物。通过与BBr3反应，将甲氧基化白杨素衍生物转化为相应的羟基化白杨素衍生物，产率较高。测定了白杨素衍生物对内毒素处理的RAW 264.7细胞产生前列腺素的抑制活性。我们发现，含有3‘，4’-二氯取代基(5E、6E和7E)的白杨素衍生物具有良好的前列腺素合成抑制活性。(C)2004爱思唯尔有限公司。保留所有权利。
A series of chrysin derivatives were prepared and evaluated for their inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin production. Chrysin derivatives were prepared from 2-hydroxyacetophenone, 2,4-dihydroxyacetophenone and 2,6-dihydroxyacetophenone in 2 to 4 steps, respectively. Methxoylated chrysin derivatives were converted to the corresponding hydroxylated chrysin derivatives by the reaction with BBr3 in good yields. The inhibitory activity of the chrysin derivatives against prostaglandin production from lipopolysaccharide-treated RAW 264.7 cells was measured. We found that chrysin derivatives with 3',4'-dichloro substituents (5e, 6e and 7e) exhibited good inhibitory activity of prostaglandin production. (C) 2004 Elsevier Ltd. All rights reserved.