Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one

被引：46

作者：

Edwards, JP

Higuchi, RI

Winn, DT

Pooley, CLF

Caferro, TR

Hamann, LG

Zhi, L

Marschke, KB

Goldman, ME

Jones, TK

机构：

[1] Dept Med Chem, San Diego, CA 92121 USA

[2] New Leads Discovery Ligand Pharmaceut, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(99)00118-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2H-pyrano[3,2-g]quinolin-2-ones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one, displayed moderate interaction with hAR, but substituted analogues were potent hAR modulators in vitro as mesaured by an hAR cotransfection assay in CV-I cells and bound to hAR with high affinity in a whole cell assay. Several analogues were able to activate hAR-mediated gene transcription more potently and efficaciously than dihydrotestosterone. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：1003 / 1008

页数：6

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