7-[Pyridin-3-yl-(pyridin-2-ylamino)methyl]quinolin-8-ol

• 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: 7-[Pyridin-3-yl-(pyridin-2-ylamino)methyl]quinolin-8-ol
• 化学式: C₂₀H₁₆N₄O
• 分子量: 328.373
• InChiKey: GQODCZOMDGLLAB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  70.9
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  3-吡啶甲醛 、 2-氨基吡啶 、 8-羟基喹啉 在 吡啶 作用下， 以 乙醇 为溶剂， 反应 0.08h， 生成 7-[Pyridin-3-yl-(pyridin-2-ylamino)methyl]quinolin-8-ol
  参考文献：
  名称：

  喹啉醇作为TEAD依赖性转录激活剂的鉴定。

  摘要：

  转录共调节因子YAP（Yes相关蛋白）和TAZ（具有PDZ结合基序的转录共激活因子）是控制各种生理和病理过程的河马信号通路的脊椎动物下游效应子。YAP和TAZ与TEAD（TEA域）家族的转录因子配对以启动转录。我们先前在TEADs中发现了一个易处理的口袋，从生理学角度来看，它可以与棕榈酸酯结合。本文中，开发了TEAD-棕榈酸酯相互作用筛选以选择占据TEAD的棕榈酸酯结合袋（PBP）的小分子。我们显示，喹啉醇是TEAD结合的化合物，可增加YAP / TAZ-TEAD活性，已通过TEAD报告基因分析，RT-qPCR和RNA-Seq分析进行了验证。结构-活性关系研究发现了TEAD激活所必需的喹啉醇取代基。我们揭示了一种新的机制，其中喹啉酚通过占据PBP来稳定YAP / TAZ蛋白水平。在小鼠伤口愈合模型中，喹啉醇提高了YAP活性，加速了体内伤口的闭合。尽管占据PBP的小分子已显示抑制YAP /

  DOI：

  10.1021/acschembio.9b00786

文献信息

• Inhibiting G Protein Coupled Receptor 6 Kinase Polypeptides
  申请人：Mayo Foundation for Medical Educational and Research

  公开号：US20140309185A1

  公开（公告）日：2014-10-16

  This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.

  这份文件涉及G蛋白偶联受体6激酶（GRK6）多肽的抑制剂，以及利用这些抑制剂治疗血液恶性肿瘤、炎症性疾病和自身免疫性疾病的方法和材料。
• Inhibiting G protein coupled receptor 6 kinase polypeptides
  申请人：Mayo Foundation for Medical Education and Research

  公开号：US10252984B2

  公开（公告）日：2019-04-09

  This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.

  本文件涉及 G 蛋白偶联受体 6 激酶（GRK6）多肽的抑制剂以及使用这种抑制剂治疗血液恶性肿瘤、炎症疾病和自身免疫性疾病的方法和材料。
• Prolylhydroxylase/ATF4 inhibitors and methods of use for treating neural cell injury or death and conditions resulting therefrom
  申请人：CORNELL UNIVERSITY

  公开号：US10716783B2

  公开（公告）日：2020-07-21

  Methods for treating a patient suffering from neural cell injury, the method comprising administering to the patient an effective amount of a HIF prolyl-4-hydroxylase inhibiting compound having the following general formula (1) wherein R1 is a cyclic group containing at least three and up to seven carbon atoms and optionally containing one or more heteroatoms selected from O, N, and S, and optionally attached to the shown carbon atom by a linking group; R2 is independently selected from said cyclic groups of R1 and acyclic hydrocarbon groups R5 containing up to twenty carbon atoms; R3 is selected from hydrogen atom and hydrocarbon groups containing up to six carbon atoms; R6 and R7 are independently selected from hydrogen atom, hydrocarbon groups containing up to three carbon atoms, halogen atom, and polar groups, as well as methylene-linked versions thereof; and t is 0 or 1.

  治疗神经细胞损伤患者的方法，该方法包括向患者施用有效量的具有下通式(1)的HIF脯氨酰-4-羟化酶抑制化合物 其中R1是含有至少三个至多七个碳原子的环状基团，任选含有一个或多个选自O、N和S的杂原子，并任选通过连接基团连接到所示碳原子；R2 独立地选自 R1 的环状基团和含有多达 20 个碳原子的无环烃基团 R5；R3 选自氢原子和含有多达 6 个碳原子的烃基团；R6 和 R7 独立地选自氢原子、含有多达 3 个碳原子的烃基团、卤素原子和极性基团及其亚甲基连接型；以及 t 为 0 或 1。
• PROLYLHYDROXYLASE/ATF4 INHIBITORS FOR TREATING NEURAL CELL INJURY
  申请人：Cornell University

  公开号：EP3079697B1

  公开（公告）日：2021-02-03
• PROLYLHYDROXYLASE/ATF4 INHIBITORS AND METHODS OF USE FOR TREATING NEURAL CELL INJURY OR DEATH AND CONDITIONS RESULTING THEREFROM
  申请人：CORNELL UNIVERSITY

  公开号：US20160317526A1

  公开（公告）日：2016-11-03

  Methods for treating a patient suffering from neural cell injury, the method comprising administering to the patient an effective amount of a HIF prolyl-4-hydroxylase inhibiting compound having the following general formula (1) wherein R 1 is a cyclic group containing at least three and up to seven carbon atoms and optionally containing one or more heteroatoms selected from O, N, and S, and optionally attached to the shown carbon atom by a linking group; R 2 is independently selected from said cyclic groups of R 1 and acyclic hydrocarbon groups R 5 containing up to twenty carbon atoms; R 3 is selected from hydrogen atom and hydrocarbon groups containing up to six carbon atoms; R 6 and R 7 are independently selected from hydrogen atom, hydrocarbon groups containing up to three carbon atoms, halogen atom, and polar groups, as well as methylene-linked versions thereof; and t is 0 or 1.