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中文摘要：
4-苯胺喹唑啉类化合物是一类具有EGFR激酶抑制活性的喹唑啉类生物碱。本文共合成了13个6位亚胺取代的4-苯胺喹唑啉类化合物,并通过MTT和Western blotting实验对其体外抗肿瘤活性进行了评价。其中化合物13a~13l是新化合物。MTT实验以人肺癌细胞株A549、肝癌细胞株Hep G2和SMMC7721为试药细胞株,结果表明化合物13i和13j对3种试药细胞株都表现出良好的抑制活性。化合物14是不含亚胺取代的4-苯胺喹唑啉,对人肺癌细胞株A549具有显著的抑制活性。通过Western blotting实验研究化合物14和13j对人肺癌细胞A549内EGFR磷酸化水平的影响,结果表明这两个化合物都能显著地抑制EGFR的磷酸化。其中化合物14的抑制强度与阳性对照gefitinib相当,而化合物13j的抑制作用强于gefitinib。
英文摘要：
Thirteen of 4-anilinoquinazoline derivatives with imine groups at position 6 of quinazoline ring were synthesized and their antitumor activities were evaluated by MTT assay and Western blotting analysis. Among these compounds, 13a-131 were reported first time. The MTT assay was carried out on three human cancer cell lines （A549, HepG2 and SMMC7721） with EGFR highly expressed. Among the tested compounds, 13i and 13j exhibited notable inhibition potency and their IC 50 values on three cell lines were equivalent to or less than those of gefitinib. Compound 14, without imine group substituted, displayed excellent inhibitor potency only on A549 cell line. Compounds 14 and 13j were chosen to perform Western blotting analysis on A549. The results showed that both of the compounds could inhibit the expression level of phosphorylated EGFR remarkably. It was concluded that the inhibitor potency of compound 14 was almost equivalent to that of gefitinib and the inhibitor potency of 13j was better than that of gefitinib.
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