Synthesis and biological evaluation of substituted 2-sulfonyl-phenyl-3-phenyl-indoles: A new series of selective COX-2 inhibitors
Synthesis and biological evaluation of substituted 2-sulfonyl-phenyl-3-phenyl-indoles: A new series of selective COX-2 inhibitors
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DOI：
10.1016/s0968-0896(03)00046-4
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发表时间：
2003-04-03
影响因子：
3.5
通讯作者：
Li, J
中科院分区：
文献类型：
--
作者：
Hu, WH;Guo, ZR;Li, J
合成了一系列新的取代2-磺基苯基-3-苯基吲哚衍生物，并对其抑制COX-2和cox -酶的能力进行了评价。大多数合成的化合物被发现是高效和选择性的COX-2抑制剂。这项工作导致2-氨基磺酰基苯基-3-苯基吲哚5a的发现，在体外和体内都比塞来昔布对COX-2具有更高的活性和选择性。2003爱思唯尔科学有限公司版权所有。
A new series of substituted 2-sulfonyphenyl-3-phenyl-indole derivatives were synthesized and evaluated for their ability to inhibit COX-2 and COX-lenzymes. Most of the compounds synthesized were found to be highly potent and selective inhibitors of COX-2. This work led to the discovery of 2-aminosulfonylphenyl-3-phenyl-indole 5a which possesses higher activity and selectivity for COX-2 than Celecoxib both in vitro and in vivo. (C) 2003 Elsevier Science Ltd. All rights reserved.