Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists

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• 作者：Steven J. Richards ; Thomas W. von Geldern ; Peer Jacobson ; Denise Wilcox ; Phong Nguyen ; Lars Ö ; hman ; Marie Ö ; sterlund ; Birgitta Gelius ; Marlena Grynfarb ; Annika Goos-Nilsson ; et al.
• 关键词：Glucocorticoids ; Cortisol ; Prednisolone ; Antagonist ; Glucocorticoid receptor ; RU-486 ; Steroid ; Bile-acid ; Liver-targeting ; Cholic acid
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 December 2006
• 卷：16
• 期：23
• 页码：6086-6090
• 文件大小：173 K

摘要

A series of potent steroidal glucocorticoid receptor antagonists has been discovered. After conjugation to cholic acid, the compounds retained an affinity for GR in vitro and had modest in vivo efficacy.