1-(4-formylphenyl)-3-(4-hydroxyphenyl)urea | 946618-56-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(4-formylphenyl)-3-(4-hydroxyphenyl)urea
• CAS: 946618-56-0
• 化学式: C₁₄H₁₂N₂O₃
• 分子量: 256.261
• InChiKey: DZKNMYWTGSSCKV-UHFFFAOYSA-N

物化性质

• 沸点：
  376.1±27.0 °C(Predicted)
• 密度：
  1.424±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.85
• 重原子数：
  19.0
• 可旋转键数：
  3.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  78.43
• 氢给体数：
  3.0
• 氢受体数：
  3.0

反应信息

• 作为反应物：
  描述：

  5,6-二甲氧基吲哚啉-2-酮 、 1-(4-formylphenyl)-3-(4-hydroxyphenyl)urea 在 哌啶 作用下， 以 乙醇 为溶剂， 以32%的产率得到C₂₄H₂₁N₃O₅
  参考文献：
  名称：

  Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones

  摘要：

  A novel series of 3-arylureidobenzylidene-indolin-2-ones was synthesized and their inhibitory activity against Ret tyrosine kinase investigated in comparison with the Ret inhibitor RPI-1 as a reference compound for this series. A few compounds were able to revert the RETC634R oncogene-transformed morphologic phenotype of NIH3T3(MEN2A) cells and showed a selective antiproliferative activity against these cells as compared to parental NIH3T3 cells or NIH3T3 cells transformed with a non-tyrosine kinase oncogene (NIH3T3(H-RAS)). Inhibition of Ret enzyme activity by effective derivatives was confirmed in a kinase assay. Structure-activity relationship indicated a favourable activity for 5,6-dimethoxyindolinone derivatives with H, OH, or OMe in the para position of the distal aryl ring. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.091
• 作为产物：
  描述：

  在 盐酸 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 生成 1-(4-formylphenyl)-3-(4-hydroxyphenyl)urea
  参考文献：
  名称：

  Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones

  摘要：

  A novel series of 3-arylureidobenzylidene-indolin-2-ones was synthesized and their inhibitory activity against Ret tyrosine kinase investigated in comparison with the Ret inhibitor RPI-1 as a reference compound for this series. A few compounds were able to revert the RETC634R oncogene-transformed morphologic phenotype of NIH3T3(MEN2A) cells and showed a selective antiproliferative activity against these cells as compared to parental NIH3T3 cells or NIH3T3 cells transformed with a non-tyrosine kinase oncogene (NIH3T3(H-RAS)). Inhibition of Ret enzyme activity by effective derivatives was confirmed in a kinase assay. Structure-activity relationship indicated a favourable activity for 5,6-dimethoxyindolinone derivatives with H, OH, or OMe in the para position of the distal aryl ring. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.091

文献信息

• Synthesis and investigation of effects of 2-[4-[[(arylamino)carbonyl]amino]phenoxy]-2-methylpropionic acids on the affinity of hemoglobin for oxygen: structure-activity relationships
  作者：Iraj Lalezari、Parviz Lalezari

  DOI：10.1021/jm00130a021

  日期：1989.10

  series of 2-[4-[[[(substituted-phenyl)amino]carbonyl]amino]phenoxy]-2- methylpropionic acids and other substituted phenoxyacetic acids were synthesized and tested for their ability to reduce the affinity of hemoglobin for oxygen. 2-[4-[[[(3,4,5-trichlorophenyl)amino]carbonyl]amino]phenoxy]-2- methylpropionic acid was found to be the most potent compound known. Structure-activity relationships of the compounds

  合成了一系列2- [4-[[[[（（取代-苯基）氨基]羰基]氨基]苯氧基] -2-甲基丙酸和其他取代的苯氧基乙酸，并测试了它们降低血红蛋白对氧的亲和力的能力。发现2- [4-[[[（（3,4,5-三氯苯基）氨基]羰基]氨基]苯氧基] -2-甲基丙酸是已知的最有效的化合物。讨论了合成化合物的构效关系。
• LALEZARI, IRAJ;LALEZARI, PARVIZ, J. MED. CHEM., 32,(1989) N0, C. 2352-2357
  作者：LALEZARI, IRAJ、LALEZARI, PARVIZ

  DOI：——

  日期：——