4-(3-Phenyl-1,8-naphthyridin-2-yl)benzaldehyde | 616870-20-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 4-(3-Phenyl-1,8-naphthyridin-2-yl)benzaldehyde
• CAS: 616870-20-3
• 化学式: C₂₁H₁₄N₂O
• 分子量: 310.355
• InChiKey: HFDIMYQUGMVXKX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(3-(piperidin-4-yl)-1H-pyrazol-5-yl)pyridine 、 4-(3-Phenyl-1,8-naphthyridin-2-yl)benzaldehyde 在 三乙酰氧基硼氢化钠 作用下， 生成 3-phenyl-2-[4-[[4-(3-pyridin-4-yl-1H-pyrazol-5-yl)piperidin-1-yl]methyl]phenyl]-1,8-naphthyridine
  参考文献：
  名称：

  Allosteric inhibitors of Akt1 and Akt2: A naphthyridinone with efficacy in an A2780 tumor xenograft model

  摘要：

  A series of naphthyridine and naphthyridinone allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been optimized to have potent dual activity against the activated kinase as well as the activation of Akt in cells. One molecule in particular, compound 17, has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.04.074
• 作为产物：
  描述：

  4-甲酰基苯硼酸 、 2-氯-3-苯基-1,8-二氮杂萘 在 caesium carbonate 作用下， 以 1,4-二氧六环 为溶剂， 以72%的产率得到4-(3-Phenyl-1,8-naphthyridin-2-yl)benzaldehyde
  参考文献：
  名称：

  Allosteric inhibitors of Akt1 and Akt2: A naphthyridinone with efficacy in an A2780 tumor xenograft model

  摘要：

  A series of naphthyridine and naphthyridinone allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been optimized to have potent dual activity against the activated kinase as well as the activation of Akt in cells. One molecule in particular, compound 17, has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.04.074

文献信息

• [EN] INHIBITORS OF AKT ACTIVITY<br/>[FR] INHIBITEURS DE L'ACTIVITÉ D'AKT
  申请人：MERCK SHARP & DOHME

  公开号：WO2010088177A1

  公开（公告）日：2010-08-05

  The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

  本发明提供了抑制Akt活性的化合物。具体而言，所披露的化合物选择性地抑制一种或两种Akt同工酶。该发明还提供了包含这些抑制性化合物的组合物以及通过向需要癌症治疗的患者施用该化合物来抑制Akt活性的方法。
• Inhibitors of akt activity
  申请人：Bilodeau T. Mark

  公开号：US20050222155A1

  公开（公告）日：2005-10-06

  The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

  本发明涉及化合物，其中包含2,3-二苯基喹喔啉基团，该基团能够抑制Akt，一种丝氨酸/苏氨酸蛋白激酶的活性。本发明还涉及包含本发明化合物的化疗组合物以及治疗癌症的方法，包括给予本发明化合物的治疗方法。
• Inhibitors of Akt activity
  申请人：Merck & Co., Inc.

  公开号：US07223738B2

  公开（公告）日：2007-05-29

  The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

  本发明涉及一种化合物，其中包含2,3-二苯基喹啉基团，可抑制Akt，一种丝氨酸/苏氨酸蛋白激酶的活性。本发明还涉及含有该发明化合物的化疗组合物以及治疗癌症的方法，包括给予该发明化合物。
• Inhibitors of AKT Activity
  申请人：Armstrong Donna J.

  公开号：US20110288090A1

  公开（公告）日：2011-11-24

  The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

  本发明提供了抑制Akt活性的化合物。特别地，所披露的化合物选择性地抑制一种或两种Akt同工型。本发明还提供了包含这种抑制剂化合物的组合物以及通过向需要癌症治疗的患者施用该化合物来抑制Akt活性的方法。
• INHIBITORS OF AKT ACTIVITY
  申请人：Merck & Co., Inc.

  公开号：EP1496896A1

  公开（公告）日：2005-01-19