Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators

被引：50

作者：

Elmore, SW ^{[1
]}

Pratt, JK

Coghlan, MJ

Mao, Y

Green, BE

Anderson, DD

Stashko, MA

Lin, CW

Falls, D

Nakane, M

Miller, L

Tyree, CM

Miner, JN

Lane, B

机构：

[1] Abbott Labs, Abbott Pk, IL 60064 USA

[2] Ligand Pharmaceut Inc, New Leads Discovery & Transcript Res, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 07期

关键词：

D O I：

10.1016/j.bmcl.2004.01.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The SAR at C-5 of the 10-methoxy-2,2,4-trimethylbenzopyrano[3,4-f]quinoline core leading to identification of (-) anti 1-methylcyclohexen-3-yl as the optimum substituent that imparts minimal GR mediated in vitro transcriptional activation while maintaining full transcriptional repression is described. The in vitro profile of these candidates in human cell assays relevant to the therapeutic window of glucocorticoid modulators is outlined. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：1721 / 1727

页数：7

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