| 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 |
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| 引用本文： | 陈贯虹,王加宁,孔学,刘可春.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[J].应用化学,2011,28(12):1375-1378. |
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| 作者姓名： | 陈贯虹 王加宁 孔学 刘可春 |
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| 作者单位： | (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) |
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| 基金项目： | 山东省国际合作资助项目 |
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| 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。
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| 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 |
| 收稿时间： | 2011-01-06 |
Synthesis and Anti-tumor Activity of 1-(4-Chloroaniline) -4-(4-pyridylmethyl) -2,3-Benzodiazine Succinate |
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| CHEN Guanhong,WANG Jianing,KONG Xue,LIU Kechun.Synthesis and Anti-tumor Activity of 1-(4-Chloroaniline) -4-(4-pyridylmethyl) -2,3-Benzodiazine Succinate[J].Chinese Journal of Applied Chemistry,2011,28(12):1375-1378. |
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| Authors: | CHEN Guanhong WANG Jianing KONG Xue LIU Kechun |
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| Institution: | (Key Laboratory of Applied Microbiology of Shandong Province,Biology Institute of Shandong Academy of Sciences,Jinan 250014) |
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| 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 tum... |
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| Keywords: | chloroaniline(pyridylmethyl)benzodiazine succinate synthesis anti-tumor activity |
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