Synthesis and Antitumor Activity of Indole Podophyllotoxin Derivatives / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize 5-substituted indole-3-deoxypodophyllotoxin derivatives and study their antitumor activity. METHODS: The target compounds were synthesized through a series of reactions and their anti-tumor activity in vitro were evaluated against Hela, K562 and K562/A02 cell lines by MTT as assay. RESULTS: Ten target compounds were synthesized and confirmed by 1H-NMR, 13C-NMR, and HR-ESI-MS. All the target compounds had different degrees of cytotoxic activity in vitro. Most of the compounds had significant anti-MDR activity in vitro. CONCLUSION: 5-Substituted indole-3-deoxypodophyllotoxin derivatives have good antitumor activity and worth of further study.