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

应用化学, 2011, 28(12): 1375-1378. doi: 10.3724/SP.J.1095.2011.00006

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 ^1, , 王加宁 ^2, , 孔学 ^3, , 刘可春 ^4,

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

2.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

3.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

4.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

基金项目: 山东省国际合作资助项目(2008GJHZ10201)

关键词：氯苯胺基(甲基吡啶基)二氮杂萘琥珀酸盐 , 化学合成 , 抑制肿瘤活性

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

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.

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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

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

参考文献