Synthesis, Crystal Structure and Anticancer Activity of Substituted Quinazoline Derivatives.

Summary: 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. [ABSTRACT FROM AUTHOR]