Synthesis and antitumor activity of tetrandrine derivatives

Abstract

Tetrandrine possesses antitumor activity, however, only a few studies on its structure modification were reported. To improve the antitumor activity of tetrandrine, 20 new tetrandrine derivatives were designed and synthesized by Sonogashira and Suzuki reactions. Their antitumor activities were evaluated against three tumor cell lines including A549, HepG2, and BGC-823 by methyl thiazolyl tetrazolium assay with taxol as a positive control. The results showed that compounds 2c and 2g were highly potent against BGC-823 cell line, and compounds 1i and 1k showed particular activity against HepG2 cells. These results demonstrated that compounds 1i, 1k, 2c, and 2g were promising leads for further investigation.

Keywords::

• tetrandrine
• derivatives
• synthesis
• bisbenzylisoquinoline alkaloid
• antitumor

Acknowledgements

The authors would like to express their sincere appreciations to Prof. Jian-Xin Li, School of Chemistry & Chemical Engineering, Nanjing University, China for his technical direction in the synthesis of the compounds.

This project was supported by the 11th Five Plan for Major Scientific and Technological Specialized Project for Significant Formulation of New Drugs (No. 2009ZX09301-007).