3-benzylidene-5-nitro-1H-indol-2-one | 1111200-38-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-benzylidene-5-nitro-1H-indol-2-one
• CAS: 1111200-38-4
• 化学式: C₁₅H₁₀N₂O₃
• 分子量: 266.256
• InChiKey: YPCNLPAUKNIQIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.09
• 重原子数：
  20.0
• 可旋转键数：
  2.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  72.24
• 氢给体数：
  1.0
• 氢受体数：
  3.0

反应信息

• 作为反应物：
  描述：

  3-benzylidene-5-nitro-1H-indol-2-one 、 ALPHA-氯-4-甲氧基苯甲醛肟 在 三乙胺 作用下， 以 氯仿 为溶剂， 反应 26.0h， 以116.5 mg的产率得到5-nitro-3'-(4-methoxyphenyl)-4'-phenylspiro[indoline-3,5'-isoxazoline]-2-one
  参考文献：
  名称：

  Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents

  摘要：

  Restoring p53 levels through disruption of p53-MDM2 interaction has been proved to be a valuable approach in fighting cancer. We herein report the synthesis and evaluation of eighteen spiroisoxazoline oxindoles derivatives as p53-MDM2 interaction inhibitors. Seven compounds showed an antiproliferative profile superior to the p53-MDM2 interaction inhibitor nutlin-3, and induced cell death by apoptosis. Moreover, proof-of-concept was demonstrated by inhibition of the interaction between p53 and MDM2 in a live-cell bimolecular fluorescence complementation assay. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2013.10.048
• 作为产物：
  描述：

  5-硝基-1,3-二氢-2H-吲哚-2-酮 、 苯甲醛 在 哌啶 作用下， 以 乙醇 为溶剂， 生成 3-benzylidene-5-nitro-1H-indol-2-one
  参考文献：
  名称：

  Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents

  摘要：

  Restoring p53 levels through disruption of p53-MDM2 interaction has been proved to be a valuable approach in fighting cancer. We herein report the synthesis and evaluation of eighteen spiroisoxazoline oxindoles derivatives as p53-MDM2 interaction inhibitors. Seven compounds showed an antiproliferative profile superior to the p53-MDM2 interaction inhibitor nutlin-3, and induced cell death by apoptosis. Moreover, proof-of-concept was demonstrated by inhibition of the interaction between p53 and MDM2 in a live-cell bimolecular fluorescence complementation assay. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2013.10.048

文献信息

• USE OF NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS
  申请人：D'Mello Santosh R.

  公开号：US20090264494A1

  公开（公告）日：2009-10-22

  The present invention include providing a therapeutically effective amount of a 3-substituted indolin-2-one compositions to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke
• USE OF NOVEL NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS
  申请人：D'Mello Santosh R.

  公开号：US20100298376A1

  公开（公告）日：2010-11-25

  The present invention provides compositions and methods of synthesizing optionally substituted 3-substituted indolin-2-ones and methods to employ the resultant compounds to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke.