期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 13, 页码 4307-4309出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.05.018
关键词
Sulfoximine; Acyclic triaryl olefin; COX-2 selective inhibitor (COXIB); Estrogen receptor
资金
- Fonds der Chemischen Industrie
- China Scholarship Council
- University of Siena
Sulfoximine-based acyclic triaryl olefins 8 and 9 have been prepared and initial studies have been performed to determine their biological profiles. In contrast to their sulfonyl-substituted analog 2 sulfoximines 8 and 9 show low COX inhibitory activity. All compounds affect the estrogen receptors. While sulfone 2 interacts exclusively with ER beta, sulfoximines 8 and 9 reveal almost equal blocking potencies for both estrogen receptors, ER alpha and ER beta. In the tested series, triaryl olefin 9a shows the highest inhibitory activities with 91% and 80%, respectively (at 10 mu M). (C) 2012 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据