本文選題：-苯胺喹唑啉 + 衍生物　； 參考：《藥學學報》2015年12期

【摘要】：4-苯胺喹唑啉類化合物是一類具有EGFR激酶抑制活性的喹唑啉類生物堿。本文共合成了13個6位亞胺取代的4-苯胺喹唑啉類化合物,并通過MTT和Western blotting實驗對其體外抗腫瘤活性進行了評價。其中化合物13a~13l是新化合物。MTT實驗以人肺癌細胞株A549、肝癌細胞株Hep G2和SMMC7721為試藥細胞株,結果表明化合物13i和13j對3種試藥細胞株都表現(xiàn)出良好的抑制活性�；衔�14是不含亞胺取代的4-苯胺喹唑啉,對人肺癌細胞株A549具有顯著的抑制活性。通過Western blotting實驗研究化合物14和13j對人肺癌細胞A549內EGFR磷酸化水平的影響,結果表明這兩個化合物都能顯著地抑制EGFR的磷酸化。其中化合物14的抑制強度與陽性對照gefitinib相當,而化合物13j的抑制作用強于gefitinib。
[Abstract]:4-aniline quinazoline compounds are a class of quinazoline alkaloids with EGFR kinase inhibitory activity.Thirteen 4-aniline quinazoline compounds were synthesized and evaluated by MTT and Western blotting in vitro.The compound 13a~13l was a new compound. MTT assay showed that compound 13i and 13j showed good inhibitory activity on three kinds of cell lines, such as human lung cancer cell line A549, hepatoma cell line Hep G2 and SMMC7721.Compound 14 is a 4-aniline quinazoline without imine substitution and has significant inhibitory activity on human lung cancer cell line A549.The effects of compounds 14 and 13j on the phosphorylation of EGFR in human lung cancer cell line A549 were studied by Western blotting assay. The results showed that both compounds could significantly inhibit the phosphorylation of EGFR.The inhibitory intensity of compound 14 was similar to that of gefitinib, while that of compound 13j was stronger than that of gefitinib.
【作者單位】： 西北大學生命科學學院西部資源與現(xiàn)代生物技術教育部重點實驗室;陜西中醫(yī)藥大學陜西省中藥資源產(chǎn)業(yè)化協(xié)同創(chuàng)新中心陜西省中藥基礎與新藥研究重點實驗室陜西省風濕與腫瘤類中藥制劑工程技術研究中心;
【基金】：Project supported by the Program for Changjiang Scholars and Innovative Research Team in University(IRT1174) the National Natural Science Foundation of China(20872118;30070905) the Key Lab Fund of Shaanxi Province of China(2010JS097;11JS090;12JS110) the Foundation of the Technology Department of Shaanxi Province(2015SF074)
【分類號】：R914;R96

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本文編號：1731956