Synthesis and anticancer activities of 5,6,7-trimethoxy-N-phenyl(ethyl)-4-aminoquinazoline derivatives

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• 作者：Ying Zhang ; Linhong Jin ; Hongmei Xiang ; Jian Wu ; Peiyi Wang ; Deyu Hu ; Wei Xue ; Song Yang
• 关键词：Quinazoline ; Anticancer ; ERK1/2 ; Antiphosphorylation ; Cell apoptosis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：August, 2013
• 年：2013
• 卷：66
• 期：Complete
• 页码：335-344
• 全文大小：981 K

文摘

A series of 5,6,7-trimethoxy-N-phenyl(ethyl)-4-aminoquinazoline compounds was prepared by microwave irradiation and conventional heating methods. Compounds 6p, 6q, and 6x strongly inhibited extracellular regulated kinase1/2 (ERK1/2) phosphorylation induced by epidermal growth factor (EGF) at 1.28?¦ÌM in PC3 cells. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay showed that all compounds had certain anticancer activities, and the IC₅₀ values of 6x were 6.2?¡À?0.9, 3.2?¡À?0.1, and 3.1?¡À?0.1?¦ÌM against PC3, BGC823, and Bcap37 cells, respectively. Acridine orange/ethidium bromide staining, Hoechst 33258 staining, DNA ladder, and flow cytometry analyses revealed that 6x induced cell apoptosis in PC3 cells, with apoptosis ratios of 11.6 % at 1?¦ÌM and 31.8 % at 10?¦ÌM after 72?h.