Discovery of novel bis-evodiamine derivatives with potent antitumor activity

Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.

Automated summary

A series of novel bis-evodiamine derivatives inspired by the antitumor natural product evodiamine were synthesized, and they exhibited potent antitumor activity. Notably, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Mechanistic studies further revealed that compound 13b induced apoptosis in HCT116 cells and arrested the cell cycle at the G2/M phase. Therefore, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.