Total synthesis and cytotoxicity evaluation of syrinenin-4-O-farnesylether and its analogues

Abstract

First synthesis of natural product, syrinenin-4-O-farnesylether (1), was carried out via two different paths. Four of its derivatives (9–12) were also prepared. Cytotoxicity screening of the selected compounds were performed on six tumour cell lines. Compound 12 exhibited prominent IC₅₀ values of 1.9 μM and 0.8 μM on CNE and PC-3 cells, respectively.

Keywords:

• Syrinenin derivative
• Syrinenin-4-O-farnesylether
• Biological activity
• Cytotoxicity

Acknowledgements

This work was financed in part by Chine-France PRA BT01-02. One of the authors (Y.Z.) would also like to express his thanks to the Chinese Ministry of Education as well as to Mr Ka-Shing Lee for a “Cheung Kong Scholar Chief Professorship” at Zhejiang University.