Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II)

Under the guidance of our previous work, we synthesized 21 new structures of quinazolines (3a similar to 3u) and evaluated their in vitro anticancer activity against A549, HCT116 and MCF-7 cell lines using the MTT method. Most compounds showed good to excellent anticancer activity. In particular, 3o (regarded as erlotinib analogues) has marked anticancer activity against A549, HCT116 and MCF-7 cell lines (IC(50)s: 4.26, 3.92 and 0.14 mu M, respectively) as compared with the standard anticancer drug gefitinib (IC(50)s: 17.9, 21.55 and 20.68 mu M, respectively), and which can be regarded as the best candidate for development of anticancer drugs.