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以N’-[5-(3-氯丙氧基)]-2-氰基-4-甲氧苯基-N,N-二甲基甲脒为原料,经过成环、醚化,合成了4个4-(3’-氯苯氨基)-6-甲氧基喹唑啉类化合物(Ⅰa～Ⅰd):N-(3’-氯苯基)-6-甲氧基-7-[3-(4-硝基苯氧基)丙氧基]喹唑啉-4-胺(Ⅰa)、N-(3’-氯苯基)-6-甲氧基-7-[3-(3-硝基苯氧基)丙氧基]喹唑啉-4-胺(Ⅰb)、4-{3-[4-(3’-氯苯胺基)-6-甲氧基喹唑啉-7-基氧基]丙氧基}-3-甲氧基苯甲醛(Ⅰc)、3-{3-[4-(3’-氯苯胺基)-6-甲氧基喹唑啉-7-基氧基]丙氧基}-4-甲氧基苯甲醛(Ⅰd),收率分别为51.3%、60.3%、85.4%、79.4%。产物的结构经IR、1HNMR、13CNMR、MS和元素分析表征。采用MTT法进行化合物抑制Bcap-37细胞的体外活性测试,结果表明,合成的化合物具有不同程度抑制Bcap-37细胞的活性,其中化合物Ⅰa在10μmol/L浓度下对Bcap-37细胞的抑制率为83.4%。
Starting from N ’- [5- (3-chloropropoxy)] -2-cyano-4-methoxyphenyl-N, N-dimethylformamidine, Four 4- (3’-chlorophenylamino) -6-methoxyquinazolines (Ia-Id): N- (3’- chlorophenyl) -6-methoxy-7- [3 (4- nitrophenoxy) propoxy] quinazolin-4-amine (Ia), N- (3’- chlorophenyl) -6-methoxy-7- [3- Nitrophenoxy) propoxy] quinazolin-4-amine (Ib), 4- {3- [4- (3’-chloroanilino) -6-methoxyquinazolin-7- Oxy] propoxy} -3-methoxybenzaldehyde (Ic), 3- {3- [4- (3’-chloroanilino) -6-methoxyquinazolin-7-yloxy ] Propoxy} -4-methoxybenzaldehyde (Id) in 51.3% yield, 60.3% yield, 85.4% yield, 79.4% yield. The structure of the product was characterized by IR, 1HNMR, 13CNMR, MS and elemental analysis. The MTT assay was used to test the inhibitory effect of the compounds on Bcap-37 cells in vitro. The results showed that the compounds inhibited the activity of Bcap-37 cells to varying degrees. The inhibitory rate of compound Ⅰa to Bcap-37 cells at 10 μmol / L was 83.4%.