5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators

被引：67

作者：

Zhi, L ^{[1
]}

Tegley, CM ^{[1
]}

Pio, B ^{[1
]}

Edwards, JP ^{[1
]}

Motamedi, M ^{[1
]}

Jones, TK ^{[1
]}

Marschke, KB ^{[1
]}

Mais, DE ^{[1
]}

Risek, B ^{[1
]}

Schrader, WT ^{[1
]}

机构：

[1] Ligand Pharmaceut Inc, Discovery Res, San Diego, CA 92121 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 19期

关键词：

D O I：

10.1021/jm020477g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5-benylidene-1,2-dihydrochromeno[3,4-f]quinolines (4) were synthesized and tested in bioassays to evaluate their progestational activities, receptor- and tissue-selectivity profiles as selective progesterone receptor modulators (SPRMs). Most of the new analogues exhibited as highly potent progestins with more than 100-fold receptor selectivity over other steroid hormone receptors and LG120920 (7b) demonstrated tissue selectivity toward uterus and vagina versus breasts in a rodent model after oral administration.

引用

页码：4104 / 4112

页数：9

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