Design and preparation of aza-analogues of benzo[c]phenanthridine framework with cytotoxic and antiplasmodial activities

Benzo[c]phenanthridine alkaloids represent interesting lead for the discovery of new potential antiplasmodial and/or anticancer drugs. In this field, a novel library of aza-analogs of benzo[c]phenanthroline framework derivatives was designed and prepared. Although these compounds did not have specific antiplasmodial activities, some of them displayed specific in vitro activity against two cancer lines especially compound 24 with an IC50 against the MCF7 line of 0.6 μM.

Graphical abstractA novel library of aza-analogs of benzo[c]phenanthroline framework derivatives was designed and prepared. All compounds were tested for in vitro antiplasmodial activities against both chloroquino-sensitive and chloroquino-resistant lines. In addition, some of them displayed good in vitro activities against two cancer lines.Figure optionsDownload full-size imageDownload as PowerPoint slide