New nonsteroidal androgen receptor modulators based on 4(trifluoromethyl)-2 (1H)-pyrrolidino[3,2-g] quinolinone

被引：72

作者：

Edwards, JP

West, SJ

Pooley, CLF

Marschke, KB

Farmer, LJ

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(98)00107-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2(1H)-pyrrolidino [3,2-g]quinolinones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g]quinolinone, displayed moderate interaction with hAR, but more substituted analogues, particularly 6,7-disubstituted compounds, were potent hAR agonists in vitro. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：745 / 750

页数：6

共 16 条

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