本文選題：-苯胺喹唑啉 + 衍生物��； 參考：《藥學(xué)學(xué)報(bào)》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(gè)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(shí)驗(yàn)對(duì)其體外抗腫瘤活性進(jìn)行了評(píng)價(jià)。其中化合物13a~13l是新化合物。MTT實(shí)驗(yàn)以人肺癌細(xì)胞株A549、肝癌細(xì)胞株Hep G2和SMMC7721為試藥細(xì)胞株,結(jié)果表明化合物13i和13j對(duì)3種試藥細(xì)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(duì)人肺癌細(xì)胞株A549具有顯著的抑制活性。通過Western blotting實(shí)驗(yàn)研究化合物14和13j對(duì)人肺癌細(xì)胞A549內(nèi)EGFR磷酸化水平的影響,結(jié)果表明這兩個(gè)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(qiáng)度與陽性對(duì)照gefitinib相當(dāng),而化合物13j的抑制作用強(qiáng)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(xué)生命科學(xué)學(xué)院西部資源與現(xiàn)代生物技術(shù)教育部重點(diǎn)實(shí)驗(yàn)室;陜西中醫(yī)藥大學(xué)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(chǔ)與新藥研究重點(diǎn)實(shí)驗(yàn)室陜西省風(fēng)濕與腫瘤類中藥制劑工程技術(shù)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(hào)】：R914;R96

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本文編號(hào)：1731956