Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents

► Pharmacomodulation of natural alkaloids to improve their profiles as anticancer agents. ► New generation of aza-analogues: benzo[c]phenanthrolines and benzo[c]phenanthrolinones. ► Introduction of dialkylaminoalkyl chains. ► Replacement of a benzene by a pyridine. ► Increased cytotoxicity and DNA affinity.