N,N'-bis-(quinolin-6-yl)-malonamide | 4354-80-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N,N'-bis-(quinolin-6-yl)-malonamide
• 英文别名: N,N'-di(quinolin-6-yl)propanediamide
• CAS: 4354-80-7
• 化学式: C₂₁H₁₆N₄O₂
• 分子量: 356.384
• InChiKey: JGVNKLGBNKLDQA-UHFFFAOYSA-N

物化性质

• 沸点：
  739.0±45.0 °C(Predicted)
• 密度：
  1.399±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  84
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-氨基喹啉 、 丙二酰氯 以 二氯甲烷 为溶剂， 反应 0.08h， 以71%的产率得到N,N'-bis-(quinolin-6-yl)-malonamide
  参考文献：
  名称：

  [EN] SUBSTITUTED 2-ARYLMETHYLENE-N-ARYL-N'-ARYL-MALONAMIDES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS
  [FR] MALONAMIDES 2-ARYLMETHYLENE-N-ARYL-N'-ARYL SUBSTITUES ET LEURS ANALOGUES UTILES COMME ACTIVATEURS DES CASPASES ET INDUCTEURS DE L'APOPTOSE

  摘要：

  公开号：

  WO2005037196A3

文献信息

• Combination methods of treating cancer
  申请人：Bacopoulos G. Nicholas

  公开号：US20070190022A1

  公开（公告）日：2007-08-16

  The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, in a first treatment procedure, and a second amount of an anti-cancer agent in a second treatment procedure. The first and second amounts together comprise a therapeutically effective amount. The effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

  本发明涉及一种治疗癌症的方法，通过在第一次治疗过程中向需要治疗的对象给予一定量的组蛋白去乙酰化酶（HDAC）抑制剂或其药学上可接受的盐或水合物，以及在第二次治疗过程中给予一定量的抗癌剂。第一次和第二次给予的药量加起来构成治疗上有效的药量。HDAC抑制剂和抗癌剂的作用可能是加成或协同的。
• Substituted 2-arylmethylene-n-aryl-n'aryl-malonamides and analogs as activators of caspases and inducers of apoptosis
  申请人：Cai Xiong Sui

  公开号：US20070043076A1

  公开（公告）日：2007-02-22

  The present invention is directed to substituted 2-arylmethylene-N-aryl-N′-aryl-malonamides and analogs thereof. The present invention also relates to the discovery that the compounds are activators of caspases and inducers of apoptosis. Therefore, the activators os caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

  本发明涉及取代的2-芳基亚甲基-N-芳基-N'-芳基-马隆酰胺及其类似物。本发明还涉及发现这些化合物是caspase的激活剂和凋亡诱导剂。因此，本发明的caspase激活剂和凋亡诱导剂可用于诱导各种临床情况下不受控制的异常细胞的生长和扩散。
• Methods of treating cancer with hdac inhibitors
  申请人：Bacopoulos G. Nicholas

  公开号：US20070060614A1

  公开（公告）日：2007-03-15

  The present invention relates to methods of treating cancers, e.g., mesothelioma or lymphoma. More specifically, the present invention relates to methods of treating mesothelioma or diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.
• [EN] SUBSTITUTED 2-ARYLMETHYLENE-N-ARYL-N'-ARYL-MALONAMIDES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS<br/>[FR] MALONAMIDES 2-ARYLMETHYLENE-N-ARYL-N'-ARYL SUBSTITUES ET LEURS ANALOGUES UTILES COMME ACTIVATEURS DES CASPASES ET INDUCTEURS DE L'APOPTOSE
  申请人：CYTOVIA INC

  公开号：WO2005037196A3

  公开（公告）日：2005-10-13