2-(4-(4-(Benzo(g)quinolin-4-ylamino)phenyl)piperazin-1-yl)ethanol | 127136-38-3

• 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: 2-(4-(4-(Benzo(g)quinolin-4-ylamino)phenyl)piperazin-1-yl)ethanol
• 英文别名: 2-[4-[4-(benzo[g]quinolin-4-ylamino)phenyl]piperazin-1-yl]ethanol
• CAS: 127136-38-3
• 化学式: C₂₅H₂₆N₄O
• 分子量: 398.5
• InChiKey: GICVXLQNOAJVLU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  51.6
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Methods and compositions for restoring conformational stability of a protein of the p53 family
  申请人：Pfizer Products Inc.

  公开号：EP1854509A2

  公开（公告）日：2007-11-14

  There is provided the use of an organic non-peptide compound that binds to one or more domains of a human protein of the p53 family under physiological conditions and stabilizes a functional conformation therein for the preparation of a medicament for promoting the activity of a human protein of the p53 family, wherein one or more functional activities of said protein are at least partially impaired by the inability of said protein to maintain a functional conformation under physiological condition. Such compound may be used in the treatment of cancer due to impaired activity of p53 family proteins (p53,p63 or p73).

  提供了一种有机非肽化合物的用途，该化合物能在生理条件下与人类 p53 家族蛋白的一个或多个结构域结合并稳定其中的功能构象，用于制备促进人类 p53 家族蛋白活性的药物，其中所述蛋白的一个或多个功能活性至少部分因所述蛋白无法在生理条件下保持功能构象而受损。这种化合物可用于治疗因 p53 家族蛋白（p53、p63 或 p73）活性受损而导致的癌症。
• METHODS AND COMPOSITIONS FOR RESTORING CONFORMATIONAL STABILITY OF A PROTEIN OF THE p53 FAMILY
  申请人：Pfizer Products Inc.

  公开号：EP1137418A2

  公开（公告）日：2001-10-04
• [EN] METHODS AND COMPOSITIONS FOR RESTORING CONFORMATIONAL STABILITY OF A PROTEIN OF THE p53 FAMILY<br/>[FR] PROCEDES ET COMPOSITIONS POUR RETABLIR LA STABILITE DE CONFORMATION D'UNE PROTEINE DE LA FAMILLE p53
  申请人：PFIZER PROD INC

  公开号：WO2000032175A2

  公开（公告）日：2000-06-08

  The invention provides pharmaceutical non-peptidic organic compounds capable of interacting with a functionally defective form of a mutant or a wild-type tumor suppressor protein of the p53 family (such as p53, p63 or p73). The interaction allows stabilization or folding of the protein in a functional conformation, thereby restoring all or part of its wild-type normal activity. More particularly said compounds interact with the DNA binding domain of p53 family proteins, are acridine, quinoline, quinazoline or phenothiazine derivatives, and are used in cancer therapy. Also provided are methods for screening such pharmacological compounds.