Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins

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• 作者：Xiao Yun Chen^a ; Seong Jun Park^a ; Helmut Buschmann^b ; Maria De Rosa^a ; ^&dagger ; ; Carsten Bolm^a ; ^{Carsten.Bolm@oc.rwth-aachen.de}
• 关键词：Sulfoximine ; Acyclic triaryl olefin ; COX-2 selective inhibitor (COXIB) ; Estrogen receptor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 July, 2012
• 卷：22
• 期：13
• 页码：4307-4309
• 文件大小：319 K

摘要

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 尾, sulfoximines 8 and 9 reveal almost equal blocking potencies for both estrogen receptors, ER 伪 and ER 尾. In the tested series, triaryl olefin 9a shows the highest inhibitory activities with 91%and 80%, respectively (at 10 渭M).