2-(1-(3-dimethylaminopropyl)-1H-indol-3-yl)-3-(1H-indol-3-yl)-N-methylmaleimide | 137592-50-8

• 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: 2-(1-(3-dimethylaminopropyl)-1H-indol-3-yl)-3-(1H-indol-3-yl)-N-methylmaleimide
• 英文别名: 2-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-N-methylmaleimide；3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)-1-methylpyrrole-2,5-dione
• CAS: 137592-50-8
• 化学式: C₂₆H₂₆N₄O₂
• 分子量: 426.518
• InChiKey: PYISNOOJRUGPGY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  61.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(1-(3-dimethylaminopropyl)-1H-indol-3-yl)-3-(1H-indol-3-yl)-N-methylmaleimide 、 N,N-二甲氨基氯丙烷盐酸盐 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以23%的产率得到
  参考文献：
  名称：

  Structure–activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors

  摘要：

  A series of N-methyl-bisindolylmaleimide derivatives was synthesized and evaluated as cell death inhibitors. N-Methyl-2[1-(3-aminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide (21) was the most potent inhibitor of H2O2-induced necrotic death of human leukemia HL60 cells among them. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.04.015
• 作为产物：
  描述：

  2,3-二氯-N-甲基马来酰亚胺顺丁烯二酰亚胺 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 生成 2-(1-(3-dimethylaminopropyl)-1H-indol-3-yl)-3-(1H-indol-3-yl)-N-methylmaleimide
  参考文献：
  名称：

  Structure–activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors

  摘要：

  A series of N-methyl-bisindolylmaleimide derivatives was synthesized and evaluated as cell death inhibitors. N-Methyl-2[1-(3-aminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide (21) was the most potent inhibitor of H2O2-induced necrotic death of human leukemia HL60 cells among them. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.04.015

文献信息

• Pyrrole derivatives and cell death inhibitors
  申请人：Sagami Chemical Research Center

  公开号：US06589977B1

  公开（公告）日：2003-07-08

  Bisindolylpyrrole derivatives represented by general formula [I] which are useful in inhibiting cell death and expected as being useful as preventives and remedies for the progress of various diseases in the progress and worsening of which cell death participates; and cell death inhibitors, drugs and cell/tissue/organ preservatives containing as the active ingredient these derivatives or pharmaceutically acceptable salts thereof.

  一般式为I的双吲哚基吡咯衍生物，在抑制细胞死亡方面非常有用，预计可作为预防和治疗参与细胞死亡的各种疾病的药物，以及含有这些衍生物或其药学上可接受的盐为活性成分的细胞死亡抑制剂、药物和细胞/组织/器官保护剂。
• CELL DEATH INHIBITORS
  申请人：SAGAMI CHEMICAL RESEARCH CENTER

  公开号：EP1057484A1

  公开（公告）日：2000-12-06

  The present invention provides cell death inhibitors comprising, as an active ingredient, an indole derivative represented by the following formula (I) which is expected as a preventive or a remedy for the progress of various diseases wherein cell death participates in progress and exacerbation thereof, drugs, preservatives for organs, tissues and cells, and assay systems using primary cultured cells:

  本发明提供了由下式（I）代表的吲哚衍生物作为活性成分组成的细胞死亡抑制剂，该活性成分可望作为预防或治疗各种疾病（细胞死亡参与了这些疾病的进展和恶化）的进展、药物、器官、组织和细胞的防腐剂以及使用原代培养细胞的检测系统：
• PYRROLE DERIVATIVES AND CELL DEATH INHIBITORS
  申请人：SAGAMI CHEMICAL RESEARCH CENTER

  公开号：EP1152002A1

  公开（公告）日：2001-11-07

  Bisindolylpyrrole derivatives represented by general formula [I] which are useful in inhibiting cell death and expected as being useful as preventives and remedies for the progress of various diseases in the progress and worsening of which cell death participates; and cell death inhibitors, drugs and cell/tissue/organ preservatives containing as the active ingredient these derivatives or pharmaceutically acceptable salts thereof.

  由通式[I]表示的双吲哚基吡咯衍生物，可用于抑制细胞死亡，并可望作为预防和治疗细胞死亡导致的各种疾病的进展和恶化的药物；以及含有这些衍生物或其药学上可接受的盐类作为活性成分的细胞死亡抑制剂、药物和细胞/组织/器官防腐剂。
• US6589977B1
  申请人：——

  公开号：US6589977B1

  公开（公告）日：2003-07-08
• [EN] METHOD FOR SUPPRESSING DIFFERENTIATION OF PLURIPOTENT STEM CELLS<br/>[FR] PROCÉDÉ POUR SUPPRIMER LA DIFFÉRENCIATION DE CELLULES SOUCHES PLURIPOTENTES<br/>[JA] 多能性幹細胞の分化抑制方法
  申请人：KANEKA CORP

  公开号：WO2021162090A1

  公开（公告）日：2021-08-19

  未分化状態を維持しながら多能性幹細胞を浮遊培養する。多能性幹細胞を浮遊培養する際に、ＰＫＣ阻害剤のなかでもＰＫＣβ阻害剤と、タンキレース阻害剤（ＴＮＫＳ阻害剤）とを存在させることで未分化状態を維持する。