Synthesis and antitumor activity of podophyllotoxin derivatives.
10.19540/j.cnki.cjcmm.20190730.201
- Author:
Dan-Li TIAN
1
;
Chun-Po LIANG
2
;
Gang LUO
3
;
Hong CHEN
3
Author Information
1. Tianjin First Central Hospital Tianjin 300192,China.
2. General Hospital of Tianjin Medical University Tianjin 300052,China.
3. Pharmacognosy Division,Medical College of Chinese People's Armed Police Force Tianjin 300309,China.
- Publication Type:Journal Article
- Keywords:
4'-demethylepipodophyllotoxin;
antitumor activity;
podophyllotoxin;
structure-activity relationship
- MeSH:
Antineoplastic Agents/pharmacology*;
Drug Design;
Drug Screening Assays, Antitumor;
Podophyllotoxin/pharmacology*;
Structure-Activity Relationship
- From:
China Journal of Chinese Materia Medica
2019;44(22):4874-4879
- CountryChina
- Language:Chinese
-
Abstract:
According to drug design flattening principle and using podophyllotoxin or 4'-demethylepipodophyllotoxin and aldehydes as starting material,a series of podophyllotoxin derivatives containing an imine structure with low toxicity were highly effective synthesized. Nine target compounds were successfully synthesized,and their structures were confirmed by ~1H-NMR,HR-ESI-MS and melting point data analysis. Using etoposide as positive control drug,nine target compounds were screened for cytotoxicity against He La cells in vitro by MTT method. The antitumor activity screening results showed that compound 6 b,6 d,6 e,6 f,6 g,6 i exhibited higher inhibitory rate against He La cells than those of control drug VP-16. It provides some practical reference value for the further development on the structure modification of podophyllotoxin and study on anti-tumor activity.
