Synthesis and anti-tumor activity of paeonol and its derivatives.
- Author:
Xue-Jun WANG
1
;
Jian-Li LIU
;
Jiang-Kai WANG
Author Information
1. Key Laboratory of Resource Biology and Biotechnology in West China, Ministry of Education, School of Life Science, Northwest University, Xi'an 710069, China.
- Publication Type:Journal Article
- MeSH:
Acetophenones;
chemical synthesis;
chemistry;
pharmacology;
Antineoplastic Agents, Phytogenic;
chemical synthesis;
chemistry;
pharmacology;
Cell Proliferation;
drug effects;
Drug Screening Assays, Antitumor;
HeLa Cells;
Humans;
Inhibitory Concentration 50;
MCF-7 Cells;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2012;47(1):72-76
- CountryChina
- Language:Chinese
-
Abstract:
A series of paeonol derivatives have been synthesized by simple acylation and etherification of the paeonol. Anti-tumor activities of the synthesized compounds were evaluated against HeLa and MCF-7 cells lines in vitro by the standard MTT assay. It was found that the derivatives were more active against HeLa than MCF-7. The results also indicated that 4-methoxy group is the synergistic group of paeonol's anti-tumor activity and ketone carbonyl side chain is essential functional group of paeonol's anti-tumor activity. Compound 2d had stronger antiproliferative activities than paeonol against HeLa and MCF-7 cell lines with IC50 values of 2.67 and 4.74 micromol x L(-1) respectively. The results showed that paeonol derivatives were worth to be intensively studied further.
