Synthesis and anticancer activities of 5,6,7-trimethoxy-N-phenyl(ethyl)-4-aminoquinazoline derivatives.
Synthesis and anticancer activities of 5,6,7-trimethoxy-N-phenyl(ethyl)-4-aminoquinazoline derivatives.
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DOI：
10.1016/j.ejmech.2013.05.043
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发表时间：
2013-08
影响因子：
6.7
通讯作者：
Ying-Xue Zhang;Linhong Jin;Hongmei Xiang;Jian Wu;Peiyi Wang;D. Hu;Wei Xue;Song Yang
中科院分区：
文献类型：
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作者：
Ying-Xue Zhang;Linhong Jin;Hongmei Xiang;Jian Wu;Peiyi Wang;D. Hu;Wei Xue;Song Yang
A series of 5,6,7-trimethoxy-N-phenyl(ethyl)-4-aminoquinazoline compounds was prepared by microwave irradiation and conventional heating methods. Compounds6p,6q, and6xstrongly inhibited extracellular regulated kinase1/2 (ERK1/2) phosphorylation induced by epidermal growth factor (EGF) at 1.28 μM in PC3 cells. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay showed that all compounds had certain anticancer activities, and the IC50values of6xwere 6.2 ± 0.9, 3.2 ± 0.1, and 3.1 ± 0.1 μM against PC3, BGC823, and Bcap37 cells, respectively. Acridine orange/ethidium bromide staining, Hoechst 33258 staining, DNA ladder, and flow cytometry analyses revealed that6xinduced cell apoptosis in PC3 cells, with apoptosis ratios of 11.6% at 1 μM and 31.8% at 10 μM after 72 h.
