indolizino[2,3-g]phthalazine-5,12-dione | 1186105-54-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: indolizino[2,3-g]phthalazine-5,12-dione
• CAS: 1186105-54-3
• 化学式: C₁₄H₇N₃O₂
• 分子量: 249.228
• InChiKey: IWXKHJQYIIDFMJ-UHFFFAOYSA-N

物化性质

• 熔点：
  >300 °C
• 密度：
  1.57±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  64.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  吡啶 、 硝基甲烷 、 6,7-二氯酞嗪-5,8-二酮 以 乙醇 为溶剂， 以7.7%的产率得到indolizino[2,3-g]phthalazine-5,12-dione
  参考文献：
  名称：

  Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors

  摘要：

  A series of novel indolizinophthalazine-5,12-dione derivatives were designed and synthesized by the reaction of 6,7-dichlorophthalazine-5,8-dione with active methylene reagents (AMR) and pyridine derivatives. Some of synthesized compounds exhibited significant in vitro antiproliferative activity at micromolar level toward four human tumor cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell and ardriamycin-resistance breast carcinoma cell. The DNA topoisomerase IB inhibitory assay indicated that DNA topoisomerase IB might be a biological target of the synthesized compounds. (C) 2010 Published by Elsevier Masson SAS.

  DOI：

  10.1016/j.ejmech.2010.05.048

文献信息

• Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors
  作者：De-Qing Shen、Zu-Ping Wu、Xi-Wei Wu、Zeng-Yun An、Xiang-Zhang Bu、Lian-Quan Gu、Zhi-Shu Huang、Lin-Kun An

  DOI：10.1016/j.ejmech.2010.05.048

  日期：2010.9

  A series of novel indolizinophthalazine-5,12-dione derivatives were designed and synthesized by the reaction of 6,7-dichlorophthalazine-5,8-dione with active methylene reagents (AMR) and pyridine derivatives. Some of synthesized compounds exhibited significant in vitro antiproliferative activity at micromolar level toward four human tumor cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell and ardriamycin-resistance breast carcinoma cell. The DNA topoisomerase IB inhibitory assay indicated that DNA topoisomerase IB might be a biological target of the synthesized compounds. (C) 2010 Published by Elsevier Masson SAS.