1-(Chinolyl-2)-3-(4-amino-phenyl)-propenon-3 | 4488-53-3

• 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: 1-(Chinolyl-2)-3-(4-amino-phenyl)-propenon-3
• 英文别名: 3-(Chinolyl-2)-1-(4-amino-phenyl)-propen-2-on-1；3-(4-Amino-phenyl)-1-(chinolyl-2)-propen-1-on-3；ACT-PFK-089；1-(4-amino-phenyl)-3-quinolin-2-yl-propenone；1-(4-Aminophenyl)-3-(2-quinolinyl)-2-propen-1-one；1-(4-aminophenyl)-3-quinolin-2-ylprop-2-en-1-one
• CAS: 4488-53-3
• 化学式: C₁₈H₁₄N₂O
• 分子量: 274.322
• InChiKey: WQJWDFPQDJWUGX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  56
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  吗啉 、 氯磺酰异氰酸酯 、 1-(Chinolyl-2)-3-(4-amino-phenyl)-propenon-3 以 甲苯 为溶剂， 反应 6.0h， 生成 1-(morpholine-4-sulfonyl)-3-[4-(3-quinolin-2-yl-acryloyl)-phenyl]-urea
  参考文献：
  名称：

  [EN] 2-PROPENE-1-ONES AS HSP 70 INDUCERS
  [FR] 2-PROPENE-1-ONES UTILISES COMME INDUCTEURS DE HSP 70

  摘要：

  公开号：

  WO2005097746A3
• 作为产物：
  描述：

  喹啉-2-甲醛 、 4-氨基苯乙酮 在 potassium hydroxide 作用下， 以 甲醇 、 水 为溶剂， 生成 1-(Chinolyl-2)-3-(4-amino-phenyl)-propenon-3
  参考文献：
  名称：

  Srinivasa Rao, Asian Journal of Chemistry, 2011, vol. 23, # 10, p. 4373 - 4376

  摘要：

  DOI：

文献信息

• 2-Propene-1-Ones As Hsp 70 Inducers
  申请人：Kumar Prabhat

  公开号：US20080207608A1

  公开（公告）日：2008-08-28

  The present invention relates to novel compounds of 2-propene-1-one series, of general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, wherein R 5 , R 6 , Q and Y are as defined in the specification. The present invention also relates to a process for preparing such compounds, compositions containing such compounds, and use of such compound and composition in medicine. The compounds of the general formula (I) induce HSP-70 and are useful for the treatment of diseases accompanying pathological stress in a living mammalian organism, including a human being, such as stroke, myocardial infarction, inflammatory disorder, hepatotoxicity, sepsis, diseases of viral origin, allograft rejection, tumourous diseases, gastric mucosal damage, brain haemorrhage, endothelial dysfunctions, diabetic complications, neuro-degenerative diseases, post-traumatic neuronal damage, acute renal failure, glaucoma and aging related skin degeneration.

  本发明涉及2-丙烯酮系列的新化合物，通式为（I），它们的衍生物，类似物，互变异构体，立体异构体，多晶形，药学上可接受的盐，药学上可接受的溶剂和含有它们的药学上可接受的组合物，其中R5，R6，Q和Y如规范中所定义。本发明还涉及制备这种化合物的过程，含有这种化合物的组合物，以及在医学上使用这种化合物和组合物。通式（I）的化合物诱导HSP-70，并用于治疗伴随病理应激的疾病，包括中风，心肌梗死，炎症性疾病，肝毒性，败血症，病毒性疾病，异体移植排斥，肿瘤性疾病，胃黏膜损伤，脑出血，内皮功能障碍，糖尿病并发症，神经退行性疾病，创伤后神经损伤，急性肾衰竭，青光眼和与衰老相关的皮肤退化。
• FAMILY OF PFKFB3 INHIBITORS WITH ANTI-NEOPLASTIC ACTIVITIES
  申请人：Tapolsky Gilles

  公开号：US20120177749A1

  公开（公告）日：2012-07-12

  A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.
• US8557823B2
  申请人：——

  公开号：US8557823B2

  公开（公告）日：2013-10-15
• [EN] METHODS OF TREATING DISEASE WITH PFKFB3 INHIBITORS<br/>[FR] MÉTHODES DE TRAITEMENT D'UNE MALADIE À L'AIDE D'INHIBITEURS DE PFKFB3
  申请人：UNIV CALIFORNIA

  公开号：WO2017208174A2

  公开（公告）日：2017-12-07

  The disclosure relates to methods for treating a protein misfolding disease in a subject comprising administering a PFKFB3 inhibitor to the subject. Further aspects relate to a method for treating or preventing protein misfolding-induced cell death in a cell, the method comprising administering a PFKFB3 inhibitor to the cell. The disclosure also describes methods for inhibiting or reducing β-cell death in a subject with Type 2 diabetes, the method comprising administering a PFKFB3 inhibitor to the subject.
• [EN] METHODS AND COMPOSITIONS FOR DIABETES TREATMENT AND BETA-CELL REGENERATION<br/>[FR] MÉTHODES ET COMPOSITIONS POUR LE TRAITEMENT DU DIABÈTE ET LA RÉGÉNÉRATION DE CELLULES BÊTA
  申请人：UNIV CALIFORNIA

  公开号：WO2022040161A1

  公开（公告）日：2022-02-24

  Aspects of the present disclosure are directed to methods and compositions for facilitating β-cell regeneration by inhibition of the HIF1α-PFKFB3 pathway. Certain aspects describe methods for treatment and prevention of prediabetes and diabetes, including type 2 diabetes. Also disclosed are methods and compositions for enhancing β-cell regeneration.