N-(3-acetylphenyl)-2-cyanoaziridine-1-carboxamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-(3-acetylphenyl)-2-cyanoaziridine-1-carboxamide
• 化学式: C₁₂H₁₁N₃O₂
• 分子量: 229.238
• InChiKey: LKHLYRDZRLHMPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  73
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  异氰酸3-乙酰基苯酯 、 2-氮丙啶甲腈 以 甲苯 为溶剂， 以74%的产率得到N-(3-acetylphenyl)-2-cyanoaziridine-1-carboxamide
  参考文献：
  名称：

  Novel Antitumor 2-Cyanoaziridine-1-carboxamides

  摘要：

  A set of 20 2-cyanoaziridine-1-carboxamides was synthesized from 2-cyanoaziridine and appropriate isocyanates. These compounds were active against a variety of solid and hematological tumor cells in culture, including strains resistant to doxorubicin and mitoxantrone. Their potencies in these assays correlated with the lipophilicity of substituents. The N-phenyl derivative was more potent and equally effective to imexon, a cyclized 2-cyanoaziridine-1-carboxamide of clinical interest, against cloned fresh human tumors.

  DOI：

  10.1021/jm980600x

文献信息

• Liposomal imexon
  申请人：——

  公开号：US20030129222A1

  公开（公告）日：2003-07-10

  Disclosed are novel compositions comprising a lipid and imexon or a derivative thereof. Also disclosed are liposomal compositions comprising imexon or a derivative thereof. Methods for administrating pharmaceutically acceptable compositions comprising a lipid and imexon or a derivative thereof for the treatment of diseases, such as cancer, are also disclosed herein.

  披露了包含脂质和伊美酮或其衍生物的新型组合物。还披露了包含伊美酮或其衍生物的脂质体组合物。本文还披露了用于治疗疾病（如癌症）的含有脂质和伊美酮或其衍生物的药用合成物的管理方法。
• NOVEL CYANOAZIRIDINES FOR TREATING CANCER
  申请人：Amplimed, Inc.

  公开号：EP1027041B1

  公开（公告）日：2003-10-22
• US6297230B1
  申请人：——

  公开号：US6297230B1

  公开（公告）日：2001-10-02
• [EN] COMPOSITION COMPRISING AN IMEXON OR DERIVATIVES THEREOF AND LIPIDS<br/>[FR] IMEXON LIPOSOMIQUE
  申请人：——

  公开号：WO2002041871A9

  公开（公告）日：2003-05-30

  [EN] Disclosed are novel compositions comprising a lipid and imexon or a derivative thereof. Also disclosed are liposomal compositions comprising imexon or derivative thereof. Methods for administrating pharmaceutically acceptable compositions comprising a lipid and imexon or a derivative thereof for the treatment of diseases, such as cancer, are also disclosed herein.
  [FR] L'invention concerne de nouvelles compositions comprenant un lipide et de l'iméxon ou un dérivé de ce dernier. L'invention traite aussi de compositions liposomiques comprenant de l'iméxon ou un dérivé de ce dernier. L'invention a aussi pour objet des procédés permettant d'administrer des compositions pharmaceutiquement acceptables comprenant un lipide et de l'iméxon ou un dérivé de ce dernier pour traiter les maladies, telles que le cancer.