• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

碳-11修饰米非司酮类似物库的合成。

Synthesis of C-11 modified mifepristone analog libraries.

作者信息

Hamilton Gregory L, Backes Bradley J

机构信息

Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.

出版信息

Mol Divers. 2007 May;11(2):107-11. doi: 10.1007/s11030-007-9058-4. Epub 2007 Jun 6.

DOI:10.1007/s11030-007-9058-4
PMID:17549597
Abstract

Substitution of the C-11 aniline of mifepristone can provide compounds with altered pharmacokinetic and pharmacodynamic (PK/PD) profiles that may find use for new indications. The development of new steroid intermediates and specialized library synthesis methods were required to enable the efficient preparation of structurally complex C-11 modified mifepristone analogs.

摘要

米非司酮C-11位苯胺的取代可提供具有改变的药代动力学和药效学(PK/PD)特征的化合物,这些化合物可能会用于新的适应症。需要开发新的甾体中间体和专门的库合成方法,以有效地制备结构复杂的C-11修饰的米非司酮类似物。

相似文献

1
Synthesis of C-11 modified mifepristone analog libraries.碳-11修饰米非司酮类似物库的合成。
Mol Divers. 2007 May;11(2):107-11. doi: 10.1007/s11030-007-9058-4. Epub 2007 Jun 6.
2
Syntheses and antigestagenic activity of mifepristone derivatives.米非司酮衍生物的合成及其抗孕激素活性。
J Med Chem. 2009 Mar 12;52(5):1268-74. doi: 10.1021/jm800985z.
3
Synthesis of 11beta-(4-dimethylaminophenyl)-17beta-hydroxy-17alpha- (3-methyl-1-butynyl)-4, 9-estradien-3-one and 11beta-(4-acetophenyl)- 17beta-hydroxy-17alpha-(3-methyl-1-butynyl)-4, 9-estradien-3-one: two new analogs of mifepristone (RU-486).11β-(4-二甲基氨基苯基)-17β-羟基-17α-(3-甲基-1-丁炔基)-4,9-雌二烯-3-酮和11β-(4-乙酰苯基)-17β-羟基-17α-(3-甲基-1-丁炔基)-4,9-雌二烯-3-酮的合成:米非司酮(RU-486)的两种新类似物
Steroids. 2000 Mar;65(3):157-62. doi: 10.1016/s0039-128x(99)00097-5.
4
Synthesis and biological evaluation of partially fluorinated antiprogestins and mesoprogestins.部分氟化抗孕激素和中孕激素的合成与生物评价。
Steroids. 2013 Feb;78(2):255-67. doi: 10.1016/j.steroids.2012.09.010. Epub 2012 Nov 21.
5
Synthesis and antihormonal properties of novel 11β-benzoxazole-substituted steroids.新型 11β-苯并恶唑取代甾体的合成及抗激素性质。
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1705-8. doi: 10.1016/j.bmcl.2011.12.110. Epub 2011 Dec 30.
6
Synthesis of a fluorescent steroid derivative with high affinities for the glucocorticoid and progesterone receptors.一种对糖皮质激素和孕激素受体具有高亲和力的荧光甾体衍生物的合成。
Steroids. 1994 Jan;59(1):22-6. doi: 10.1016/0039-128x(94)90040-x.
7
Synthesis, spectral characterization, and in vitro cellular activities of metapristone, a potential cancer metastatic chemopreventive agent derived from mifepristone (RU486).米非司酮(RU486)衍生的潜在癌症转移化学预防剂美普清的合成、光谱特征及体外细胞活性。
AAPS J. 2014 Mar;16(2):289-98. doi: 10.1208/s12248-013-9559-2. Epub 2014 Jan 18.
8
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.新型氧杂甾体作为孕酮受体拮抗剂的合成与鉴定
Bioorg Med Chem Lett. 2007 Feb 15;17(4):907-10. doi: 10.1016/j.bmcl.2006.11.062. Epub 2006 Dec 1.
9
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists.
Bioorg Med Chem Lett. 2008 Jul 15;18(14):3852-5. doi: 10.1016/j.bmcl.2008.06.059. Epub 2008 Jun 20.
10
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.肝靶向糖皮质激素受体拮抗剂的制备与筛选并行策略
Bioorg Med Chem Lett. 2007 Jan 1;17(1):40-4. doi: 10.1016/j.bmcl.2006.10.001. Epub 2006 Oct 5.

本文引用的文献

1
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.肝脏选择性糖皮质激素拮抗剂:2型糖尿病的一种新型治疗方法。
J Med Chem. 2004 Aug 12;47(17):4213-30. doi: 10.1021/jm0400045.
2
Steroids and combinatorial chemistry.类固醇与组合化学。
J Comb Chem. 2004 Jul-Aug;6(4):443-56. doi: 10.1021/cc030118m.
3
The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism.糖皮质激素受体配体结合域的拮抗和激动形式的三维结构:RU-486诱导一种导致活性拮抗作用的反式构象。
J Biol Chem. 2003 Jun 20;278(25):22748-54. doi: 10.1074/jbc.M212711200. Epub 2003 Apr 9.
4
RU486 (mifepristone): mechanisms of action and clinical uses.RU486(米非司酮):作用机制及临床应用
Annu Rev Med. 1997;48:129-56. doi: 10.1146/annurev.med.48.1.129.
5
Regio and stereospecific synthesis of 11 beta-substituted 19-norsteroids. Influence of 11 beta-substitution on progesterone receptor affinity - (1).
Steroids. 1981 Apr;37(4):361-82. doi: 10.1016/0039-128x(81)90039-8.
6
Pharmacokinetic properties of the antiglucocorticoid and antiprogesterone steroid RU 486 in man.
J Pharmacol Exp Ther. 1987 May;241(2):401-6.