Design, synthesis, and biological evaluation of (E)- and (Z)-styryl-2-acetoxyphenyl sulfides and sulfones as cyclooxygenase-2 inhibitors
Design, synthesis, and biological evaluation of (E)- and (Z)-styryl-2-acetoxyphenyl sulfides and sulfones as cyclooxygenase-2 inhibitors
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DOI：
10.1016/j.bmc.2004.12.005
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发表时间：
2005-03-01
影响因子：
3.5
通讯作者：
Reddy, EP
中科院分区：
文献类型：
--
作者：
Reddy, MVR;Mallireddigari, MR;Reddy, EP
设计并合成了一系列具有（E）-和（Z）-构型的苯乙烯基乙酰氧基苯硫醚和砜。所有这些化合物都进行了体外抑制考克斯-2酶的能力评价。构效关系研究表明，只有（Z）-构型的硫醚具有潜在的考克斯-2抑制活性。这种酶的失活被认为是由于抑制剂对考克斯-2的选择性共价修饰。(C)2004爱思唯尔有限公司保留所有权利。
A new series of styryl acetoxyphenyl sulfides and sulfones possessing (E)- and (Z)-configurations were designed and prepared by stereospecific syntheses. All these compounds were evaluated for their ability to inhibit COX-2 enzyme in vitro. Structure-activity relationship studies on these compounds revealed that only sulfides with (Z)-configuration have potential COX-2 inhibitory activity. This inactivation of the enzyme is believed to be due to the selective covalent modification of COX-2 by the inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.