Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.

作者信息

Regan John, Lee Thomas W, Zindell Renée M, Bekkali Younes, Bentzien Jörg, Gilmore Thomas, Hammach Abdelhakim, Kirrane Thomas M, Kukulka Alison J, Kuzmich Daniel, Nelson Richard M, Proudfoot John R, Ralph Mark, Pelletier Josephine, Souza Donald, Zuvela-Jelaska Lijiljana, Nabozny Gerald, Thomson David S

机构信息

Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA.

出版信息

J Med Chem. 2006 Dec 28;49(26):7887-96. doi: 10.1021/jm061273t.

DOI:10.1021/jm061273t

PMID:17181172

Abstract

We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.

摘要

相似文献

Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.

J Med Chem. 2006 Dec 28;49(26):7887-96. doi: 10.1021/jm061273t.

Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.

J Med Chem. 2007 Dec 27;50(26):6519-34. doi: 10.1021/jm070778w. Epub 2007 Nov 27.

Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.

J Med Chem. 2010 Sep 23;53(18):6681-98. doi: 10.1021/jm100751q.

Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.

J Med Chem. 2006 Jul 13;49(14):4216-31. doi: 10.1021/jm060302x.

Identification of dissociated non-steroidal glucocorticoid receptor agonists.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5025-31. doi: 10.1016/j.bmcl.2007.07.031. Epub 2007 Jul 25.

Selective prostacyclin receptor agonism augments glucocorticoid-induced gene expression in human bronchial epithelial cells.

J Immunol. 2009 Nov 15;183(10):6788-99. doi: 10.4049/jimmunol.0902738. Epub 2009 Oct 30.

Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.

J Med Chem. 2004 May 6;47(10):2441-52. doi: 10.1021/jm030585i.

Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6842-51. doi: 10.1016/j.bmcl.2011.09.018. Epub 2011 Sep 10.

Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5199-203. doi: 10.1016/j.bmcl.2004.07.052.

Molecular mechanisms of glucocorticoid action and selective glucocorticoid receptor agonists.

Mol Cell Endocrinol. 2007 Sep 15;275(1-2):71-8. doi: 10.1016/j.mce.2007.05.019. Epub 2007 Jun 2.

引用本文的文献

Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

ACS Med Chem Lett. 2014 Nov 20;5(12):1318-23. doi: 10.1021/ml500387y. eCollection 2014 Dec 11.

Pharmacomimetics of exercise: novel approaches for hippocampally-targeted neuroprotective agents.

Curr Med Chem. 2009;16(35):4668-78. doi: 10.2174/092986709789878292.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型，支持多种主流文档格式。

立即体验