Synthesis, in vitro and in vivo evaluation of novel substituted N-(4-(2-(4-benzylpiperazin-1-yl)ethoxy)phenyl)-N-methyl-quinazolin-4-amines as potent antitumor agents

Abstract A novel series of substituted N -(4-(2-(4-benzylpiperazin-1-yl)ethoxy)phenyl)- N -methylquinazolin-4-amines were synthesized and evaluated for their in vitro antiproliferative activity. Among them, compound 7a exhibited the best potency, with IC 50 values of 0.029–0.147 μM against four types of cancer cell lines. In addition, 7a was confirmed that it could arrest the cell cycle at G 2 /M phase and trigger apoptosis. Indirect immunofluorescence staining revealed its anti-tubulin property. Importantly, 7a significantly inhibited tumor growths in HepG2 xenograft models without causing significant loss of body weight, suggesting that 7a is a promising new anticancer agent to be developed.