A series of 1-azaaurone derivatives were designed and synthesized from 3,5-dimethoxyaniline and 2-chloroacetonitrile. Their structures were characterized by melting point, 1 H NMR, IR, and elemental analysis, as well as 13 C NMR. The target compounds were evaluated for antitumor activities against human hepatocellular liver carcinoma cell line (HepG-2) and human cervix carcinoma cell line (Hela) using methyl thiazolyl tetrazolium method. The results revealed that several 1-azaaurones exhibited strong proliferation inhibition efficacy against HepG-2 and Hela with an IC 50 range of 5.6-8.8 μg/mL without damaging normal cell.
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