Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists

被引：8

作者：

Biggadike, Keith ^{[1
]}

Caivano, Matilde ^{[1
]}

Clackers, Margaret ^{[1
]}

Coe, Diane M. ^{[1
]}

Hardy, George W. ^{[1
]}

Humphreys, Davina ^{[1
]}

Jones, Haydn T. ^{[1
]}

House, David ^{[1
]}

Miles-Williams, Annette ^{[1
]}

Skone, Philip A. ^{[1
]}

Uings, Iain ^{[1
]}

Weller, Vicki ^{[1
]}

McLay, Iain M. ^{[1
]}

Macdonald, Simon J. F. ^{[1
]}

机构：

[1] GlaxoSmithKline Inc, Resp CEDD, Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

Glucocorticoid; Agonist; Non-steroidal; Tractable; MODULATORS; DISCOVERY; FUROATE;

D O I：

10.1016/j.bmcl.2009.06.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NF kappa B agonist activity was optimised in an iterative process from pIC(50) 7.5 (for 7), to pIC(50) 10.1 (for 38E1). An explanation for the SAR observed based is presented along with a proposed docking of 38E1 into the active site of the glucocorticoid receptor. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4846 / 4850

页数：5

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