Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators

被引:20
作者
Zhi, L [1 ]
Tegley, CM [1 ]
Pio, B [1 ]
Edwards, JP [1 ]
Jones, TK [1 ]
Marschke, KB [1 ]
Mais, DE [1 ]
Risek, B [1 ]
Schrader, WT [1 ]
机构
[1] Ligand Pharmaceut, Discovery Res, San Diego, CA 92121 USA
关键词
D O I
10.1016/S0960-894X(03)00255-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 5-methylidene 1,2-dihydrochromeno[3,4-]quinoline derivatives were synthesized and tested in biological assays to evaluate scope and limitations of the nonsteroidal SPRM pharmacophore (3). A number of orally available highly potent nonsteroidal modulators were identified by modification of the substituents at 5-methylidene position. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2071 / 2074
页数:4
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