Relationship between cytotoxicity and DNA-binding affinity of amidine derivatives of tetrahydroquino[4,3-b][1]benzazepines and tetrahydrobenzo[k]naphthyridines

Two sets of amidine derivatives of the non-planar tetracyclic systems: tetrahydroquino[4.3-b][1]benzazepine (I) and tetrahydrobenzo[k]naphthyridine (II), bearing three types of side chains (hydroxyl, amine and alkyl) have been synthesized. All the compounds were found to possess weak but significant DNA-binding affinity which correlated with in vitro cytotoxicity across two cell lines.