This study identifies potential antitumor compounds from a series of new stigmasterol derivatives. Eleven stigmasterol derivatives were synthesized and their structures were confirmed by 1H NMR, MS, and elemental analyses. Their cytotoxicity in vitro against three human cancer cell lines (MCF-7, A549 and HepG2) were evaluated by the MTT assay. Among these compounds, AB-5 and AB-11 shows much better cytotoxicity against MCF-7, A549, and HepG2 cells, and AB-10 exhibits selective cytotoxicity against MCF-7. Their structure–activity relationships were also investigated. In conclusion, AB-5, AB-10 and AB-11 serve as potential compounds for the new generation of anticancer drugs.

Yu Lu, Jizhi Hu, Zibin Wu, Li Zeng and Bo Yu