4-alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono [5,6-g]quinolines:: Potent, nonsteroidal androgen receptor agonists

被引：49

作者：

Higuchi, RI

Edwards, JP

Caferro, TR

Ringgenberg, JD

Kong, JW

Hamann, LG

Arienti, KL

Marschke, KB

Davis, RL

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 | 1999年 / 9卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(99)00186-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of human androgen receptor (hAR) agonists based on 4-alkyl-: 4,4-dialkyl-; and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono [5,6-g] quinoline was synthesized and evaluated In competitive receptor binding assays and an androgen receptor cotransfection assay in a mammalian cell background. A number of compounds in this series demonstrated activity equal to or better than dihydrotestosterone in both assays and represent a novel class of compounds for use in androgen replacement therapy. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：1335 / 1340

页数：6

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