5(Z)-Benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators

被引：12

作者：

Ardecky, Robert J. ^{[1
]}

Hudson, Andrew R. ^{[1
]}

Phillips, Dean P. ^{[1
]}

Tyhonas, John S. ^{[1
]}

Deckhut, Charlotte ^{[1
]}

Lau, Thomas L. ^{[1
]}

Li, Yongkai ^{[1
]}

Martinborough, Esther A. ^{[1
]}

Roach, Steven L. ^{[1
]}

Higuchi, Robert I. ^{[1
]}

Lopez, Francisco J. ^{[1
]}

Marschke, Keith B. ^{[1
]}

Miner, Jeffrey N. ^{[1
]}

Karanewsky, Donald S. ^{[1
]}

Negro-Vilar, Andres ^{[1
]}

Zhi, Lin ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 15期

关键词：

glucocorticoid; hormone receptor; cortisol; inflammation; prednisolone; dexamethasone;

D O I：

10.1016/j.bmcl.2007.05.062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5-benzylidene-1,2-dihydro-2,2,4-trimetbyl-5H-1-aza-6-oxa-chrysenes was synthesized and profiled for their ability to act as selective glucocorticoid receptor modulators (SGRMs). The synthesis and structure-activity relationships for this series of compounds are presented. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4158 / 4162

页数：5

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