N-((8-hydroxyquinolin-7-yl)(p-tolyl)methyl)benzamide

• 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: N-((8-hydroxyquinolin-7-yl)(p-tolyl)methyl)benzamide
• 英文别名: N-[(8-Hydroxyquinolin-7-YL)(4-methylphenyl)methyl]benzamide；N-[(8-hydroxyquinolin-7-yl)-(4-methylphenyl)methyl]benzamide
• 化学式: C₂₄H₂₀N₂O₂
• 分子量: 368.435
• InChiKey: KISDJXZVLXBGQQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  8-羟基喹啉 、 对甲基苯甲醛 、 苯甲酰胺 反应 3.0h， 以16%的产率得到N-((8-hydroxyquinolin-7-yl)(p-tolyl)methyl)benzamide
  参考文献：
  名称：

  Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

  摘要：

  使用Betti反应高效生成2OG氧化酶抑制剂，包括KDM4去甲基酶。

  DOI：

  10.1039/c5cc06095h

文献信息

• MITOCHONDRIAL TRIFUNCTIONAL PROTEIN (MTP) INHIBITORS FOR USE IN THE TREATMENT OF HIGH MITOCHONDRIAL RESPIRATION (OX+) CANCERS
  申请人：UNIVERSITE DE BORDEAUX

  公开号：EP3501540A1

  公开（公告）日：2019-06-26

  The present invention describes the identification of two cancer sub-groups based on their bioenergetics status: high mitochondrial respiration (OX+) and low mitochondrial respiration (OX-). Advantageously, it has been discovered that inhibition of the mitochondrial trifunctional protein (MTP) altered high mitochondrial respiration (OX+) tumor growth in vitro and in vivo. Hence, the present invention relates to MTP inhibitor for use in the treatment of high mitochondrial respiration (OX+) cancers. It has also been established that high mitochondrial respiration (OX+) cancer cells use an energy source other than glucose such as fatty acids for their growth, survival and resistance to treatments or activation of metastatic processes. These cancers are hence high fatty-acid oxidation dependent (FAO+) cancers. The present invention thus also relates to MTP inhibitor or use in the treatment of high mitochondrial respiration (OX+) cancers and high fatty-acid oxidation (FAO+) cancers. It has also been determined that MTP expression in tumors allows determining the prognosis of a subject suffering from high mitochondrial respiration (OX+) cancers.

  本发明描述了根据生物能状态确定的两种癌症亚群：高线粒体呼吸（OX+）和低线粒体呼吸（OX-）。有利的是，已发现抑制线粒体三功能蛋白（MTP）可改变高线粒体呼吸（OX+）肿瘤在体外和体内的生长。 因此，本发明涉及用于治疗高线粒体呼吸（OX+）癌症的 MTP 抑制剂。此外，已证实高线粒体呼吸（OX+）癌细胞使用葡萄糖以外的能量来源，如脂肪酸，以促进其生长、存活、抵抗治疗或激活转移过程。因此，这些癌症是高脂肪酸氧化依赖性（FAO+）癌症。因此，本发明还涉及 MTP 抑制剂或用于治疗高线粒体呼吸（OX+）癌症和高脂肪酸氧化（FAO+）癌症。此外，还确定了肿瘤中 MTP 的表达可用于确定高线粒体呼吸（OX+）癌症患者的预后。
• [EN] METHODS OF TREATMENT USING WNT INHIBITORS<br/>[FR] PROCÉDÉS DE TRAITEMENT UTILISANT DES INHIBITEURS DE WNT
  申请人：UNIV UTAH RES FOUND

  公开号：WO2010014948A1

  公开（公告）日：2010-02-04

  Described herein are methods of treating a cancer mediated by a Wnt signaling pathway, with a variety of compounds, including Wnt inhibitor compounds. Also described are methods of identifying compounds capable of modulating a Wnt signaling pathway.