a School of Pharmacy, Second Military Medical University, Shanghai 200433, China;
b Department of Radiation Oncology, Ji'nan Military General Hospital, Jinan 250031, China
Abstract:
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.