2-(喹啉-4-基)乙酰胺 | 10147-05-4

• 物质功能分类: 医药中间体 - 喹啉类化合物
• 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
• 中文名称: 2-(喹啉-4-基)乙酰胺
• 英文名称: 2-quinolin-4-yl-acetamide
• 英文别名: [4]quinolyl-acetic acid amide；[4]Chinolyl-essigsaeure-amid；2-(Quinolin-4-YL)acetamide；2-quinolin-4-ylacetamide
• CAS: 10147-05-4
• 化学式: C₁₁H₁₀N₂O
• mdl: MFCD11109970
• 分子量: 186.213
• InChiKey: GOGCURMGXYPPRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  56
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933499090

反应信息

• 作为反应物：
  描述：

  2-(喹啉-4-基)乙酰胺 在 盐酸 作用下， 生成 2-(喹啉-4-基)乙酸乙酯
  参考文献：
  名称：

  制备喹啉基和吡啶基乙酸酯的新方法。

  摘要：

  DOI：

  10.1002/ardp.19572900505
• 作为产物：
  描述：

  4-喹啉乙酸 在 氨 、 N,N'-羰基二咪唑 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 2-(喹啉-4-基)乙酰胺
  参考文献：
  名称：

  Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region

  摘要：

  A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34 nM to > 20 mu M and were dependant upon both the nature of the aryl group and the hydrogen bond donating potential of the maleimide ring. Key interactions with the kinase ATP site and hinge region were found to be consistent with homology modeling predictions. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.02.059

文献信息

• INHIBITORS OF JUN N-TERMINAL KINASE
  申请人：SHAM Hing L.

  公开号：US20130072494A1

  公开（公告）日：2013-03-21

  The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, C a , C b , Z, R 5 , W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.

  本公开提供了具有以下结构的c-Jun N端激酶（JNK）抑制剂： 或其盐或溶剂，其中环A、Ca、Cb、Z、R5、W和Cy在此被定义。本公开还提供了包括本公开化合物的药物组合物以及制备和使用本公开化合物和组合物的方法，例如，在治疗和预防各种疾病，如阿尔茨海默病中使用。
• Inhibitors of Jun N-Terminal Kinase
  申请人：Sham Hing L.

  公开号：US20100331335A1

  公开（公告）日：2010-12-30

  The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, C a , C b , Z, R 5 , W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.

  本公开提供抑制c-Jun N-末端激酶（JNK）的抑制剂，其结构符合以下公式：其中环A、Ca、Cb、Z、R5、W和Cy在此定义。本公开还提供包括本公开化合物的药物组合物以及制备和使用本公开化合物和组合物的方法，例如在治疗和预防各种疾病，如阿尔茨海默病中的应用。
• Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors
  作者：Guoxin Zhu、Scott Conner、Xun Zhou、Chuan Shih、Harold B. Brooks、Eileen Considine、Jack A. Dempsey、Cathy Ogg、Bharvin Patel、Richard M. Schultz、Charles D. Spencer、Beverly Teicher、Scott A. Watkins

  DOI：10.1016/s0960-894x(03)00133-1

  日期：2003.4

  A novel series of pyrrolo[3,4-c] carbazoles fused with a quinolinyl/isoquinolinyl moiety were synthesized and their D1/CDK4 inhibitory and antiproliferative activity were evaluated. Compound 8H, 14H-isoquinolinyl[6,5-a]-pyrrolo[3,4-c]carbazole-7,9-dione (1d) was found to be a highly potent D1/CDK4 inhibitor with an IC50 of 69 nM. Compound Id also inhibited tumor cell growth, arrested tumor cells in G1 phase and inhibited pRb phosphorylation. (C) 2003 Elsevier Science Ltd. All rights reserved.
• US8450363B2
  申请人：——

  公开号：US8450363B2

  公开（公告）日：2013-05-28
• US9073891B2
  申请人：——

  公开号：US9073891B2

  公开（公告）日：2015-07-07