Design, synthesis and biological evaluation of E-ring modified evodiamine derivatives as novel antitumor agents

A series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Their capacity to interfere with the catalytic activity of topoisomerase I and II was evaluated by the relaxation assay. In vitro antitumor activity results revealed that compound 12 showed good antitumor activity with a broad spectrum. Its binding modes with topoisomerase I and II were clarified by molecular docking.

Graphical abstractA series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Compound 12 showed good antitumor activity with a broad spectrum, which acted by dual inhibition of topoisomerase I and II.Figure optionsDownload full-size imageDownload as PowerPoint slide