Synthesis and in vitro evaluation of 3-substituted-1-azaanthraquinones

In the course of developing novel antitumor agents, we synthesized 3-substituted-1-azaanthraquinones, incorporating the alkylating or latent alkylating substituents as potential antitumor agents. The most active comound 4 exhibited cytotoxic activity comparable to that of doxorubicin. The compounds 3–8 retained much of their activity against the doxorubicin-resistant cell line (MCF7/R).