Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines

被引:25
作者
Hamann, LG
Winn, DT
Pooley, CLF
Tegley, CM
West, SJ
Farmer, LJ
Zhi, L
Edwards, JP
Marschke, KB
Mais, DE
Goldman, ME
Jones, TK
机构
[1] Ligand Pharmaceut Inc, Dept Med Chem, San Diego, CA 92121 USA
[2] Ligand Pharmaceut Inc, Dept New Leads Discovery, San Diego, CA 92121 USA
[3] Ligand Pharmaceut Inc, Dept Endocrine Res, San Diego, CA 92121 USA
关键词
D O I
10.1016/S0960-894X(98)00482-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of nonsteroidal human progesterone receptor (hPR) antagonists based on conformationally-restricted analogues of a 6-aryl-1,2-dihydro-2,2,4-trimethylquinoline pharmacophore were synthesized and evaluated for their ability to bind to the human progesterone receptor and inhibit progesterone-stimulated reporter gene expression in mammalian cells, (C) 1998 Elsevier Science Ltd. AU rights reserved.
引用
收藏
页码:2731 / 2736
页数:6
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