4-苯胺喹唑啉衍生物的合成及抗EGFR活性研究（英文）

发布时间：2018-04-10 16:13

本文选题：-苯胺喹唑啉 + 衍生物　；参考：《药学学报》2015年12期

【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。
[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.
【作者单位】：西北大学生命科学学院西部资源与现代生物技术教育部重点实验室;陕西中医药大学陕西省中药资源产业化协同创新中心陕西省中药基础与新药研究重点实验室陕西省风湿与肿瘤类中药制剂工程技术研究中心;
【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)
【分类号】：R914;R96

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