Synthesis and antiproliferative activity of 9-benzylamino-6-chloro-2-methoxy-acridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors

A series of 9-benzyl acridine derivatives were synthesized and evaluated as good antiproliferative inhibitors. All of them displayed strong Topo II inhibitory activity at 100 μM. The typical compound 8p showed potent DNA-binding ability, caused DNA double-strand breaks and induced A549 cells apoptosis through caspase-dependent intrinsic pathway.158