3-[1-(3-hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-(1-naphthalenyl)-1H-pyrrole-2,5-dione | 626603-95-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 3-[1-(3-hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-(1-naphthalenyl)-1H-pyrrole-2,5-dione
• 英文别名: 3-[1-(3-Hydroxy-propyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-naphthalen-1-yl-pyrrole-2,5-dione；3-[1-(3-hydroxypropyl)pyrrolo[2,3-b]pyridin-3-yl]-4-naphthalen-1-ylpyrrole-2,5-dione
• CAS: 626603-95-0
• 化学式: C₂₄H₁₉N₃O₃
• 分子量: 397.433
• InChiKey: RLESTJQOEHIBLM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  84.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-[1-(3-hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-(1-naphthalenyl)-1H-pyrrole-2,5-dione 在 吡啶 作用下， 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：

  在 盐酸 作用下， 生成 3-[1-(3-hydroxypropyl)-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

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。
• 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。
• Treatment of pluripotent cells
  申请人：Janssen Biotech, Inc.

  公开号：EP2664669A1

  公开（公告）日：2013-11-20

  The present invention is directed to methods to treat pluripotent cells, whereby the pluripotent cells can be efficiently expanded in culture and differentiated by treating the pluripotent cells with an inhibitor of GSK-3B enzyme activity.

  本发明涉及处理多能细胞的方法，通过用 GSK-3B 酶活性抑制剂处理多能细胞，可有效地扩增培养多能细胞并使其分化。
• TREATMENT OF PLURIPOTENT CELLS
  申请人：Janssen Biotech, Inc.

  公开号：EP2664669B1

  公开（公告）日：2017-12-27
• Treatment of Pluripotent Cells
  申请人：Janssen Biotech, Inc.

  公开号：US20140080210A1

  公开（公告）日：2014-03-20

  The present invention is directed to methods to treat pluripotent cells, whereby the pluripotent cells can be efficiently expanded in culture and differentiated by treating the pluripotent cells with an inhibitor of GSK-3B enzyme activity.