(E)-9-methoxy-11H-indeno[1,2-c]quinolin-11-one oxime | 1239489-17-8

• 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: (E)-9-methoxy-11H-indeno[1,2-c]quinolin-11-one oxime
• CAS: 1239489-17-8
• 化学式: C₁₇H₁₂N₂O₂
• 分子量: 276.294
• InChiKey: BMHPBSHDFOHGDN-HTXNQAPBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.45
• 重原子数：
  21.0
• 可旋转键数：
  1.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  54.71
• 氢给体数：
  1.0
• 氢受体数：
  4.0

反应信息

• 作为产物：
  描述：

  6-chloro-9-methoxy-11H-indeno[1,2-c]quinolin-11-one 在 盐酸羟胺 作用下， 以 乙醇 为溶剂， 反应 48.5h， 生成 (E)-9-methoxy-11H-indeno[1,2-c]quinolin-11-one oxime
  参考文献：
  名称：

  Discovery of Indeno[1,2-c]quinoline Derivatives as Inhibitors of Osteoclastogenesis Induced by Receptor Activator of NF-κB Ligand (RANKL)

  摘要：

  Certain indeno[1,2-c]quinolines were synthesized and evaluated for antiosteoclastogenic activities. Among them, 6,9-dimethoxy-11H-indeno[1,2-c]quinolin-11-one (8a) and 9-methoxy-6-(methylthio)-11H-indeno[1,2-c]quinolin-11-one (16a) inhibited RANKL-induced osteoclast formation in Raw 264.7 cells with an IC50 of 2.00 and 2.58 mu M, respectively. Compound 8a was only weakly active in the inhibition of the: RANKL-induced NFAT activation; while 16a was inactive. These results indicated that the antiosteoclastogenic effect of 8a is only; partly related while 16a is not related to the suppression of NFAT.

  DOI：

  10.1021/jm1016494

文献信息

• Imino-Indeno[1,2-c] quinoline derivatives, their preparation processes, and pharmaceutical compositions comprising the same
  申请人：Tzeng Cherng-Chyi

  公开号：US20090111987A1

  公开（公告）日：2009-04-30

  Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives, their synthetic precursors and their uses in the manufacture of pharmaceutical compositions for use in the treatment of cancers.

  本文披露了一种新型的imino-indeno[1,2-c]quinoline衍生物，其化学式为(I)：或其药用可接受的盐或溶剂，其中每个取代基的定义如规范和权利要求所述。还披露了这些衍生物的制备过程、它们的合成前体以及它们在制造用于治疗癌症的药物组合物中的用途。
• US7829567B2
  申请人：——

  公开号：US7829567B2

  公开（公告）日：2010-11-09
• Discovery of Indeno[1,2-<i>c</i>]quinoline Derivatives as Inhibitors of Osteoclastogenesis Induced by Receptor Activator of NF-κB Ligand (RANKL)
  作者：Chih-Hua Tseng、Ru-Wei Lin、Yeh-Long Chen、Gwo-Jaw Wang、Mei-Ling Ho、Cherng-Chyi Tzeng

  DOI：10.1021/jm1016494

  日期：2011.4.28

  Certain indeno[1,2-c]quinolines were synthesized and evaluated for antiosteoclastogenic activities. Among them, 6,9-dimethoxy-11H-indeno[1,2-c]quinolin-11-one (8a) and 9-methoxy-6-(methylthio)-11H-indeno[1,2-c]quinolin-11-one (16a) inhibited RANKL-induced osteoclast formation in Raw 264.7 cells with an IC50 of 2.00 and 2.58 mu M, respectively. Compound 8a was only weakly active in the inhibition of the: RANKL-induced NFAT activation; while 16a was inactive. These results indicated that the antiosteoclastogenic effect of 8a is only; partly related while 16a is not related to the suppression of NFAT.