One-pot synthesis of novel antiproliferative 9-aminoacridines

Highly efficient one-pot syntheses of antiproliferative 9-aminoacridine (9-AA) derivatives are described. Simple S_NAr and addition/elimination reactions, using readily accessible starting materials, give a fast entry to novel 9-(pyridylamino)acridines, 9-(pyrimidinylamino) acridines and potential "dual-function" bioreductive 9-(acridinylamino)quinone intercalators. The synthetic routes reported in this work are general and readily applicable, significantly expanding the range and scope of potential 9-AA anticancer candidates.