3-[3-(4-Naphthalen-1-yl-2,5-dioxopyrrol-3-yl)pyrrolo[2,3-b]pyridin-1-yl]propyl methanesulfonate | 729609-96-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 3-[3-(4-Naphthalen-1-yl-2,5-dioxopyrrol-3-yl)pyrrolo[2,3-b]pyridin-1-yl]propyl methanesulfonate
• CAS: 729609-96-5
• 化学式: C₂₅H₂₁N₃O₅S
• 分子量: 475.525
• InChiKey: FPSVEKBXBDWTPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  116
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  二甲胺 、 3-[3-(4-Naphthalen-1-yl-2,5-dioxopyrrol-3-yl)pyrrolo[2,3-b]pyridin-1-yl]propyl methanesulfonate 以 四氢呋喃 为溶剂， 生成 3-[1-[3-(dimethylamino)propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-(1-naphthalenyl)-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：

  {1-[3-(tert-Butyl-dimethyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-oxo-acetic acid methyl ester 在 吡啶 、 盐酸 、 potassium tert-butylate 作用下， 以 四氢呋喃 为溶剂， 生成 3-[3-(4-Naphthalen-1-yl-2,5-dioxopyrrol-3-yl)pyrrolo[2,3-b]pyridin-1-yl]propyl methanesulfonate
  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：Zhang Han-Cheng

  公开号：US20090181982A1

  公开（公告）日：2009-07-16

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

  本发明涉及一种新的取代吡咯烷化合物，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。
• US7524858B2
  申请人：——

  公开号：US7524858B2

  公开（公告）日：2009-04-28
• US7705015B2
  申请人：——

  公开号：US7705015B2

  公开（公告）日：2010-04-27
• US7781450B2
  申请人：——

  公开号：US7781450B2

  公开（公告）日：2010-08-24
• US7786135B2
  申请人：——

  公开号：US7786135B2

  公开（公告）日：2010-08-31