Synthesis and biological evaluation of dialkylaminoalkylamino benzo[c][1,7] and [1,8]phenanthrolines as antiproliferative agents

Benzo[c][1,7] and [1,8]phenanthroline substituted by dialkylaminoalkyl side chains at position C2 and C1, respectively, were synthesized and their biological activity evaluated. These compounds displayed more potent cytotoxicity toward L1210 cells than the parent unsubstituted compounds, associated with strong DNA interaction. The moderate TopoI inhibitory activity induced by the novel compounds suggests that other cellular targets should be responsible for the antiproliferative activity.

Figure optionsDownload as PowerPoint slide