Synthesis Of Imidazo[1,2-F]Phenanthridine Derivatives Under A Metal- And Base-Free Condition And Their Anticancer Activity

A series of imidazo[1,2-f]phenanthridine derivatives were synthesized from phenanthridin-6-amine and aldehydes through sulfur endorsed oxidative cyclization reaction under a metal- and base-free condition with atom economy strategy and evaluated their anticancer activity. Among all the synthesized derivatives, the compound 3d and 3f exhibited IC50 values of 2.18 +/- 0.08 and 2.24 mu M +/- 0.71 mu M, respectively. Compound 3d had the strongest inhibitory activity against HT-29 cells with an IC50 value being 1.25 mu M +/- 0.22 mu M, which was even stronger than that of paclitaxel. (C) 2021 Elsevier Ltd. All rights reserved.