News series of substituted quinazoline derivatives has been synthesized from 3,4-dihydro-7-methoxy-4-oxoquinazoline-6-yl acetate (1) by five-step procedures including chlorination, amination, hydrolysis and etherification. The structures of target compounds were confirmed by IR, 1H-NMR, element analysis and single-crystal X-ray diffraction. The results showed that the compound 8c exhibited remarkable inhibitory activity against MCF-7 cell lines with inhibition rate value of 38.45 %, which was comparable to that of the positive control Gefitinib (inhibition rate = 13.25 % for MCF-7). The initial relationship between structure and activity was worth further exploration.

Bo Wang, Zhi-qiang Cai, Xiao-yu Shi, Xiang Li, Shuai Li, and Ji-xin Li