Discovery and optimization of 7-aminofuro2,3-cpyridine inhibitors of TAK1

HornbergerK.R.; BergerD.M.; CrewA.P.DongH.KleinbergA.LiA.-H.MedeirosM.R.MulvihillM.J.SiuK.TarrantJ.WangJ.WengF.WildeV.L.AlbertellaM.BittnerM.CookeA.GrayM.J.MarescaP.MayE.MeynP.PeickJr.W.RomashkoD.TanowitzM.TokarB.

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Discovery and optimization of 7-aminofuro2,3-cpyridine inhibitors of TAK1

【24h】

Discovery and optimization of 7-aminofuro2,3-cpyridine inhibitors of TAK1

机译：TAK1的7-氨基呋喃并2,3-c吡啶抑制剂的发现与优化

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

The discovery and potency optimization of a series of 7-aminofuro2,3-c pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to ～10 nM, as exemplified by compound 12az. Application of structure-based drug design aided by co-crystal structures of TAK1 with inhibitors significantly shortened the number of iterations required for the optimization.

机译：描述了一系列 TAK1 的 7-氨基呋喃并[2,3-c] 吡啶抑制剂的发现和效力优化。从高通量筛选中提取的微摩尔命中物针对生化和细胞机制效力进行了优化，达到 ~10 nM，如化合物 12az 所示。在TAK1与抑制剂的共晶结构辅助下，应用基于结构的药物设计，大大缩短了优化所需的迭代次数。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2013年第16期|4517-4522|共6页
作者
HornbergerK.R.; BergerD.M.; CrewA.P.DongH.KleinbergA.LiA.-H.MedeirosM.R.MulvihillM.J.SiuK.TarrantJ.WangJ.WengF.WildeV.L.AlbertellaM.BittnerM.CookeA.GrayM.J.MarescaP.MayE.MeynP.PeickJr.W.RomashkoD.TanowitzM.TokarB.;
展开▼
作者单位

OSI Pharmaceuticals LLC, 1 Bioscience Park Drive, Farmingdale, NY 11735, United States;

展开▼
收录信息
原文格式 PDF
正文语种英语
中图分类药学;
关键词
7-Amino-furo2; 3-cpyridine; Cancer; Inflammation; Inhibitors; TAK1;

机译：7-氨基呋喃并[2;3-c]吡啶;巨蟹座;炎症;抑制剂;TAK1型;

相似文献

外文文献
中文文献
专利

1. Discovery of a potent and highly selective transforming growth factor beta receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD) [J] . Muraoka Terushige, Ide Mitsuaki, Morikami KenjiIrie MachikoNakamura MitsuakiMiura TakaakiKamikawa TakayukiNishihara MasamichiKashiwagi Hirotaka Bioorganic and medicinal chemistry . 2016,第18期

机译：Discovery of a potent and highly selective transforming growth factor beta receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD)
2. Spiro(imidazo(1,2-a)pyrano(2,3-c)pyridine-9-indenes) as inhibitors of gastric acid secretion. [J] . Palmer AM, Chrismann S, Munch G Bioorganic and medicinal chemistry . 2009,第1期

机译：Spiro(imidazo(1,2-a)pyrano(2,3-c)pyridine-9-indenes) as inhibitors of gastric acid secretion.
3. Glucose-6-phosphatase catalytic enzyme inhibitors: synthesis and in vitro evaluation of novel 4,5,6,7-tetrahydrothieno(3,2-c)- and -(2,3-c)pyridines. [J] . Madsen P, Lundbeck JM, Jakobsen PVarming ARWestergaard N Bioorganic and medicinal chemistry . 2000,第9期

机译：Glucose-6-phosphatase catalytic enzyme inhibitors: synthesis and in vitro evaluation of novel 4,5,6,7-tetrahydrothieno(3,2-c)- and -(2,3-c)pyridines.

Discovery and optimization of 7-aminofuro2,3-cpyridine inhibitors of TAK1

摘要

著录项

相似文献

相关主题

期刊订阅