Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy

被引：41

作者：

Thompson, CF

Quraishi, N

Ali, A

Tata, JR

Hammond, ML

Balkovec, JM

Einstein, M

Ge, L

Harris, G

Kelly, TM

Mazur, P

Pandit, S

Santoro, J

Sitlani, A

Wang, CL

Williamson, J

Miller, DK

Yamin, TTD

Thompson, CM

O'Neill, EA

Zaller, D

Forrest, MJ

Carballo-Jane, E

Luell, S

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Immunol, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Pharmacol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 08期

关键词：

glucocorticoid; dissociation; transrepression; transactivation; inflammation;

D O I：

10.1016/j.bmcl.2005.02.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2163 / 2167

页数：5

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