Synthesis and cytotoxic activities of podophyllotoxin derivatives / 中草药

Objective: To modify the structure of podophyllotoxin derivatives and evaluate the antitumor activities of the derivatives. Methods: The target compounds were synthesized by multi-step reaction with podophyllotoxin and aldehyde compound as starting material.. MTT assay was used to test antitumor activity of all the target compounds on Hela cells, K562 cells, and K562/A02 cell. Results: Eleven novel derivatives were synthesized which had not been reported in any literature and the structures were characterized by 1H-NMR, 13C-NMR, HR-ESI-MS and melting point determination analysis. The antitumor activity screening results showed that all the target compounds had different degrees of cytotoxic activity in vitro. Most of the compounds had significant anti-MDR activity in vitro. Conclusion: Through structural modification of podophyllotoxin derivatives, the antineoplastic activities are enhanced.

Synthesis and antitumor activity of novel indole podophyllotoxin derivatives / 中国中药杂志

According to drug design flattening principle,a series of novel indole podophyllotoxin derivatives which were introduced different indole substituents in C-4 position on the basis of podophyllotoxin nucleus were synthesized with the starting material podophyllotoxin and 1 H-indole-5-carboxylic acid. Its anti-tumor activity in vitro was tested in order to screen for high-efficiency and low-toxic compounds. Six target compounds were synthesized,and were confirmed by~1 H-NMR,~(13)C-NMR,HR-ESI-MS and melting point determination analysis. All these target compounds were not reported by previous literature. Using etoposide as positive control drug,all the target compounds were screened for cytotoxicity against He La cells,K562 cells and K562/A02 cell in vitro by MTT method. The antitumor activity screening results showed that compounds 4 b,4 e,4 f exhibited higher inhibitory rate against He La cells and K562 cells than those of control drug VP-16. This route has the advantages on simple operation and reasonable design,provides some practical reference value for the further development on the structure modification of podophyllotoxin and study on anti-tumor activity.

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

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.