Design, synthesis and biological evaluation of 4-amino-quinolines as antitumor agents

Fifteen novel 4-amino-quinolines (I-1-III3) as antitumor agent were synthesized by p-nitroaniline and ethoxymethylene malonic ester (EMME) via condensation, cyclization, hydrolysis, decarboxylation, chlorination, nucleophilic substitution, reduction and amidation. The antitumor activity of compounds I-1-III3 was evaluated on SGC-7901, BEL-7402 and A549 cancer cell lines. In vitro bioassay indicated that some compounds showed different degree activity against all tested cancer cell lines. Compound I-1, I-4 and II (2) exhibited high effects against A549 cell lines (IC50 = 1.34 mu M, 1.36 mu M and 3.00 mu M, respectively). In addition, the result of molecular docking showed that compound I-1, I-4 and II (2) could dock into the pocket of EGFR.