Synthesis and anti-tumor activity evaluation of novel podophyllotoxin derivatives

In order to investigate the effects on the cytotoxicity of indole-3-oxalylamino podophyllotoxin analogs, seven novel podophyllotoxin derivatives were synthesized. The compounds were tested against Hela, K562 or K562/A02 cancer cells in vitro, four of which showed significant cytotoxicity. Among them 9a, 9b and 9c were superior to the positive control VP-16.

Based on the medical chemistry combination principles, seven novel C4-N-substituted novel podophyllotoxin derivatives were synthesized. Among them, several analogs showed an improved anti-tumor activity than podophyllotoxin.Figure optionsDownload as PowerPoint slide