Jie Ren, Juan Zhao, Yong Zhou
Oct 30, 2012
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Journal
Medicinal Chemistry Research
Abstract
A series of novel 4-aminoquinoline derivatives were synthesized as antitumor agents by reacting 4-chloroquinoline with the corresponding mono/dialkyl amines. The cytotoxicity of these compounds was evaluated in vitro against HCT-116, A549, DU-145, HepG2, and LN229 cell lines. The results showed that most of the synthesized compounds displayed excellent cytotoxicity, and 5,7-dimethoxy-2-phenyl-N-propylquinoline-4-amine (6a) displayed the most potent cytotoxicity against HCT-116 cells. Furthermore, 6a could decrease VEGF protein expression.Graphical abstractThe synthesis and antitumor activity of 4-aminoquinoline derivatives have been described.