| 高宏亮,王留昌,徐宏江,张喜全,刘仁杰,李宝林.化学通报,2014,77(10):974-979. |
| 新型喹唑啉类化合物的合成与抗癌活性的初步研究 |
| The Synthesis of Novel 4-Arylaminoquinazolne Derivatives and Primary Study on Anti-tumor Activity |
| 投稿时间：2014-01-03 修订日期：2014-02-12 |
| DOI： |
| 中文关键词: 香兰素 4-芳氨基喹唑啉 喹唑啉 抗肿瘤活性 |
| 英文关键词:vanillin , 4-arylaminoquinazoline, quinazoline, anti-tumor activity |
| 基金项目:国家自然科学基金项目（面上项目，重点项目，重大项目） |
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| 中文摘要: |
| 以香兰素为起始原料,经过氰基化、醚化、硝化、还原、和环化反应,合成了一系列新型的含二苯乙烯结构单元的4-芳胺基喹唑啉类衍生物。化合物的结构经IR,1H-NMR和13C-NMR测试确证,并采用MTT法对SMMC-7721(人肝癌细胞)、MDA-MB-231(人乳腺癌细胞)、SK-OV-3(人卵巢癌细胞)等几种常见肿瘤细胞进行了初步体外抗肿瘤活性实验。结果表明合成的化合物均具有良好的抑制肿瘤细胞生长的作用。 |
| 英文摘要: |
| The desired novel 4-arylaminoquinazolne derivatives were prepared from vanillin as the starting material by a step procedures of conversion including aldehyde to nitrile, nitration, reduction, reaction with DMF-DMA to give a formamidine intermediate, and finally cyclization with arylamines via Dimroth rearrangement. Their structures were characterized with IR, 1H-NMR and 13C-NMR. The anti-tumor activities of these compounds were tested preliminarily on SMMC-7721, MDA-MB-231, SK-OV-3 and other cells by the MTT method in vitro experiment. The results indicated that these compounds possess better anti-tumor effects. |
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