{1-[3-(tert-Butyl-dimethyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-oxo-acetic acid methyl ester | 626604-78-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: {1-[3-(tert-Butyl-dimethyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-oxo-acetic acid methyl ester
• CAS: 626604-78-2
• 化学式: C₁₉H₂₈N₂O₄Si
• 分子量: 376.528
• InChiKey: DVPJBFJQWSKORK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  26.0
• 可旋转键数：
  7.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  70.42
• 氢给体数：
  0.0
• 氢受体数：
  6.0

反应信息

• 作为反应物：
  描述：

  {1-[3-(tert-Butyl-dimethyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-oxo-acetic acid methyl ester 在 盐酸 、 potassium tert-butylate 作用下， 以 四氢呋喃 为溶剂， 生成 3-(2-chlorophenyl)-4-[1-(3-hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-1H-pyrrole-2,5-dione
  参考文献：
  名称：

  3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3

  摘要：

  A novel series of acyclic 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides was synthesized and evaluated for activity against GSK-3beta and selectivity versus PKC-betaII, as well as a broad panel of protein kinases. Compounds 14 and 17c potently inhibited GSK-3beta (IC50=7 and 26nM, respectively) and exhibited excellent selectivity over PKC-betaII (325 and >385-fold, respectively). Compound 17c was also highly selective against 68 other protein kinases. In a cell-based functional assay, both 14 and 17c effectively increased glycogen synthase activity by inhibiting GSK-3beta. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.03.090
• 作为产物：
  描述：

  7-氮杂吲哚 在 乙基溴化镁 、 caesium carbonate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 生成 {1-[3-(tert-Butyl-dimethyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-oxo-acetic acid methyl ester
  参考文献：
  名称：

  3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3

  摘要：

  A novel series of acyclic 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides was synthesized and evaluated for activity against GSK-3beta and selectivity versus PKC-betaII, as well as a broad panel of protein kinases. Compounds 14 and 17c potently inhibited GSK-3beta (IC50=7 and 26nM, respectively) and exhibited excellent selectivity over PKC-betaII (325 and >385-fold, respectively). Compound 17c was also highly selective against 68 other protein kinases. In a cell-based functional assay, both 14 and 17c effectively increased glycogen synthase activity by inhibiting GSK-3beta. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.03.090

文献信息

• Substituted pyrroline kinase inhibitors
  申请人：——

  公开号：US20040006095A1

  公开（公告）日：2004-01-08

  The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.

  本发明涉及新型取代吡咯烯化合物，可用作激酶抑制剂，并用于治疗或改善激酶介导的疾病的方法。