Synthesis and biological activities of 10-substituted benzo[b][1,5]naphthyridines

Eight 10-substituted benzo[b][1,5]naphthyridine derivatives containing N-(pyrrolidino)alkylamines, methanesulfonanilides, and aminoacetanilides were prepared, and their binding with DNA was studied by (a) Tm measurements and (b) the effect on DNA-dependent RNA polymerase in vitro. In addition, they were evaluated as antineoplastic agents in the P-388 test. None of the compounds exhibited anti-cancer activity.