应用化学 ›› 2011, Vol. 28 ›› Issue (12): 1375-1378.DOI: 10.3724/SP.J.1095.2011.00006

• 研究论文 • 上一篇    下一篇

1-(4-氯苯胺基)-4-(4-吡啶甲基)-2,3-二氮杂萘琥珀酸盐的合成与抑制肿瘤活性

陈贯虹,王加宁*,孔学,刘可春   

  1. (山东省科学院生物研究所,山东省应用微生物重点实验室 济南 250014)
  • 收稿日期:2011-01-06 修回日期:2011-03-21 出版日期:2011-12-10 发布日期:2011-12-10
  • 通讯作者: 王加宁, 研究员; Tel:0531-82605925; Fax:0531-82965634; E-mail:wangjn@keylab.net; 研究方向:药物化学
  • 基金资助:
    山东省国际合作资助项目(2008GJHZ10201)

Synthesis and Anti-tumor Activity of 1-(4-chloro Chloroaniline)-4-(4-pyridylmethyl)- 2,3-Benzodiazine Succinate

CHEN Guanhong, WANG Jianing*, KONG Xue, LIU Kechun   

  1. (Key Laboratory of Applied Microbiology of Shandong Province,Biology Institute of Shandong Academy of Sciences,Jinan 250014)
  • Received:2011-01-06 Revised:2011-03-21 Published:2011-12-10 Online:2011-12-10

摘要:

研究了1-(4-氯苯胺基)-4-(4-吡啶甲基)-2,3-二氮杂萘琥珀酸盐的合成工艺,采用苯酞和吡啶甲醛为起始原料,经加成、重排、取代和成盐4步反应得到目标化合物。 中间体及目标化合物通过1H NMR、MS和HPLC进行了表征。 重结晶纯化后的目标化合物纯度为98.1%。 对荷瘤(人大肠癌HT 29细胞)裸鼠的抑癌活性测定表明,该化合物具有明显的抑制肿瘤生长作用。

关键词: 氯苯胺基(吡啶甲基)二氮杂萘琥珀酸盐, 化学合成, 抑制肿瘤活性

Abstract:

1-(4-Chloroaniline)-4-(4-pyridylmethyl)-2,3-benzodiazine succinate(4) was synthesized by addition, rearrangement, substitution and halogenesis steps with phthalide and 4-pyridinecarbaldehydes as starting reagents. The intermediate and target compound 4 were characterized by 1H NMR, MS and HPLC. After purification by recrystallization, the compound 4(98.1% purity estimated by HPLC) was experimentally used to treat colorectal cancer nude mice. The result shows that this compound obviously restrains the growth of tumors.

Key words: chloroaniline(pyridylmethyl)benzodiazine succinate, chemical synthesis, Anti-tumor activity

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