N-[(5-chloro-8-hydroxyquinolin-7-yl)-(furan-2-yl)methyl]pyridine-3-carboxamide

• 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: N-[(5-chloro-8-hydroxyquinolin-7-yl)-(furan-2-yl)methyl]pyridine-3-carboxamide
• 化学式: C₂₀H₁₄ClN₃O₃
• 分子量: 379.8
• InChiKey: NOSJDLVTDMTHKP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  27
• 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：
  88.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] INHIBITORS OF JMJD2C AS ANTICANCER AGENTS<br/>[FR] INHIBITEURS DE JMJD2C UTILISÉS EN TANT QU'AGENTS ANTICANCÉREUX
  申请人：DAVID GLADSTONE INST

  公开号：WO2015167874A1

  公开（公告）日：2015-11-05

  The present disclosure provides compounds, pharmaceutical compositions and related methods for the treatment of cancer, e.g., castration-resistant prostate cancer (CRPC). Specifically, the present disclosure provides a series of 8-hydroxyquinoline derivatives which show cytotoxic effects on androgen-independent prostate cancer cells.

  本公开提供了化合物、制药组合物和相关方法，用于治疗癌症，例如去势抵抗性前列腺癌（CRPC）。具体而言，本公开提供一系列8-羟基喹啉衍生物，其对雄激素非依赖性前列腺癌细胞具有细胞毒性作用。
• INHIBITORS OF JMJD2C AS ANTICANCER AGENTS
  申请人：The J. David Gladstone Institutes

  公开号：EP3137079A1

  公开（公告）日：2017-03-08
• Mechanism-based inhibitors of transthyretin amyloidosis: studies with biphenyl ethers and structural templates
  申请人：Surolia Avadhesha

  公开号：US20100190832A1

  公开（公告）日：2010-07-29

  Transthyretin (TTR), a tetrameric thyroxine (T4) carrier protein, is associated with a variety of amyloid diseases. Derivative of biphenyl ethers (BPE), which are shown to interact with a high affinity to its T4 binding site thereby preventing its aggregation and fibrillogenesis. They prevent fibrillogenesis by stabilizing the tetrameric ground state of transthyretin. Two compounds (2-(5-mercapto-[1,3,4]oxadiazol-2-yl)-phenol and 2,3,6-trichloro-N-(4H-[1,2,4]triazol-3-yl) exhibit the ability to arrest TTR amyloidosis. The dissociation constants for the binding of BPEs and compound 11 and 12 to TTR correlate with their efficacies of inhibiting amyloidosis. They also have the ability to inhibit the elongation of intermediate fibrils as well as show nearly complete (>90%) disruption of the preformed fibrils. Biphenyl ethers and compounds 11 and 12 as very potent inhibitors of TTR fibrillization and inducible cytotoxicity.
• Inhibitors of JMJD2C as Anticancer Agents
  申请人：The J. David Gladstone Institutes

  公开号：US20170044107A1

  公开（公告）日：2017-02-16

  The present disclosure provides compounds, pharmaceutical compositions and related methods for the treatment of cancer, e.g., castration-resistant prostate cancer (CRPC). Specifically, the present disclosure provides a series of 8-hydroxyquinoline derivatives which show cytotoxic effects on androgen-independent prostate cancer cells.