Synthesis and cytotoxic activities of podophyllotoxin derivatives
10.7501/j.issn.0253-2670.2019.18.005
- Author:
Dan-Li TIAN
1
Author Information
1. Tianjin First Central Hospital
- Publication Type:Journal Article
- Keywords:
Antitumor activity;
Cytotoxic activities;
Derivatives;
Podophyllotoxin;
Structure modification;
Structure-activity relationship
- From:
Chinese Traditional and Herbal Drugs
2019;50(18):4281-4287
- CountryChina
- Language:Chinese
-
Abstract:
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.
