Aromatic β-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists
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- 作者：Yongli Du ; Qunyi Li ; Bing Xiong ; Xin Hui ; Xin Wang ; Yang Feng ; Tao Meng ; Dingyu Hu ; Datong Zhang ; Mingwei Wang ; Jingkang Shen
- 关键词：Progesterone receptor (PR) ; Progesterone receptor antagonist ; Non-steroidal progesterone receptor antagonist ; Aromatic β ; -amino-ketone ; Mannich reaction
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2010
- 出版时间：15 June 2010
- 年：2010
- 卷：18
- 期：12
- 页码：4255-4268
- 全文大小：925 K
文摘
A novel class of non-steroidal progesterone receptor antagonists with aromatic β-amino-ketone scaffold have been synthesized and characterized with high binding affinity and great selectivity for the cognate receptors. Among them, compound 22 was shown to be the most potent progesterone receptor antagonist in cotransfection assay and a murine model of ligand-induced decidualization.