4-苯胺喹唑啉类化合物的合成与抗癌活性初步研究  

Syntheses of 4-Quinazoline Derivatives and Primary Study of Their Anti-Tumor Activity

作　　者：高宏亮[1] 王留昌[1] 徐宏江 张喜全 刘仁杰[1] 李宝林[1] 

机构地区：[1]教育部药用资源与天然药物化学重点实验室陕西师范大学化学化工学院,西安710062 [2]正大天晴药业集团股份有限公司,南京210038

出　　处：《化学通报》2014年第10期974-979,共6页Chemistry

基　　金：国家自然科学基金项目(21272144)资助

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确证,并采用MTT法对SMMC-7721(人肝癌细胞)、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。Nine kinds of 4-arylaminoquinazoline derivative were prepared using vanillin as the starting material by a step procedures of conversion including eyanation, nitration, reduction, reaction with DMF-DMA, and finally cyelization with arylamines via Dimroth rearrangement. Their structures were characterized with IR, 1H NMR and 13C NMR. The anti-tumor activities of these compounds on SMMC-7721, SK-OV-3 and some other cells were tested preliminarily by the MTT method in vitro experiment. The results indicated that these compounds possess good antitumor effects.

关 键 词：香兰素 4-芳氨基喹唑啉 喹唑啉 抗肿瘤活性 

分 类 号：O626.323[理学—有机化学] TQ460.1[理学—化学]