3-Amino-5H-pyrido(4,3-b)indole | 69901-70-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-Amino-5H-pyrido(4,3-b)indole
• 英文别名: 5H-pyrido[4,3-b]indol-3-amine
• CAS: 69901-70-8
• 化学式: C₁₁H₉N₃
• 分子量: 183.21
• InChiKey: OVNVUPPLRLREBY-UHFFFAOYSA-N

物化性质

• 沸点：
  306.89°C (rough estimate)
• 密度：
  1.2078 (rough estimate)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54.7
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• [EN] AZAINDOLE COMPOUNDS AS HISTONE METHYLTRANSFERASE INHIBITORS<br/>[FR] COMPOSÉS D'AZAINDOLE UTILISÉS EN TANT QU'INHIBITEURS D'HISTONE MÉTHYLTRANSFÉRASE
  申请人：GLOBAL BLOOD THERAPEUTICS INC

  公开号：WO2018226998A1

  公开（公告）日：2018-12-13

  The present disclosure provides certain angular tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本公开提供了一些特定的角三环化合物，它们是组蛋白甲基转移酶G9a和/或GLP抑制剂，因此可用于治疗通过抑制G9a和/或GLP可治疗的疾病，如癌症和血红蛋白病（例如β地中海贫血和镰状细胞病）。还提供了含有这些化合物的药物组合物和制备这些化合物的方法。
• Methods and diagnostic kits utilizing mammalian stress promoters to determine toxicity of a compound
  申请人：President and Fellows of Harvard College and Xenometrix, Inc.

  公开号：US20030219714A1

  公开（公告）日：2003-11-27

  This invention provides methods and diagnostic kits for identifying and characterizing toxic compounds. These methods and diagnostic kits measure transcription or translation levels from genes linked to native eukaryotic stress promoters, especially those of mammals. The kits and methods of this invention utilize at least one stress promoter from each of the following groups: redox stress, DNA stress, protein stress and energy/ionic stress. The invention also provides methods and diagnostic kits for identifying and characterizing compounds that are toxic to specific organs, such as skin and the eye, as well as for each of the individual stresses indicated above. The methods and diagnostic kits of this invention yield information concerning the action of a compound on a subcellular level. This information may be utilized to design antitoxins to compounds found to be toxic and in active drug design.

  本发明提供了识别和鉴定有毒化合物的方法和诊断试剂盒。这些方法和诊断试剂盒可测量与原生真核生物应激启动子（尤其是哺乳动物的应激启动子）相连的基因的转录或翻译水平。本发明的试剂盒和方法利用了至少一种来自以下各组的应激启动子：氧化还原应激、DNA 应激、蛋白质应激和能量/离子应激。本发明还提供了一些方法和诊断试剂盒，用于识别和鉴定对特定器官（如皮肤和眼睛）有毒的化合物，以及上述每种应激。本发明的方法和诊断试剂盒可获得化合物在亚细胞水平上的作用信息。这些信息可用于设计抗毒素，以对抗被发现具有毒性的化合物，也可用于活性药物的设计。
• METHODS AND DIAGNOSTIC KITS UTILIZING MAMMALIAN STRESS PROMOTERS TO DETERMINE TOXICITY OF A COMPOUND
  申请人：PRESIDENT AND FELLOWS OF HARVARD COLLEGE

  公开号：EP0680517B1

  公开（公告）日：1997-11-12
• AZAINDOLE COMPOUNDS AS HISTONE METHYLTRANSFERASE INHIBITORS
  申请人：Global Blood Therapeutics, Inc.

  公开号：EP3634962A1

  公开（公告）日：2020-04-15
• Multi-stage stem cell carcinogenesis
  申请人：Krtolica Ana

  公开号：US20100162416A1

  公开（公告）日：2010-06-24

  The present invention relates to a system of multi-stage stem cell carcinogenesis and a method of generating such multi-stage stem cell carcinogenesis system. Various stages of cancer stem cells can be generated from normal stem cells via mutagenesis. The system of the present invention enables monitoring changes in the ability of cells to transition from one stage of carcinogenesis to another and to identify genetic pathways and molecules that influence carcinogenesis. The present invention also enables a high-throughput and nonbiased screening for targets that preferentially affect cancer stem cells relative to non-cancer stem cells or their derivatives during stem cell carcinogenesis, thus is useful in developing anti-cancer therapeutics.