Anti-hepatitis B virus and anti-cancer activities of novel isoflavone analogs

We have synthesized a series of novel isoflavone analogs and evaluated their anti-HBV and anti-cancer activities in vitro. The bioassays showed that the majority of the resultant compounds exerted inhibitory effects on HBsAg and HBeAg levels, HBV DNA replication, as well as the growth of four human cancer cell lines to various extents, which supported the rationale of the design. In particular, compound 8f showed the highest activity against HBV infection and HBV-related liver cancer. Compound 7l (IC50 = 0.47 μM) also exerted remarkable inhibitory effect on the growth lung cancer cell line A-549.

Graphical abstractA series of novel isoflavone analogs were synthesized for developing a drug with the ability to cure patients with HBV and to treat HBV-induced HCC simultaneously.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► We synthesized a series of novel isoflavone analogs. ► Heck reaction was employed. ► All resultant compounds were evaluated for their in vitro anti-HBV activities. ► All resultant compounds were evaluated for their in vitro cytotoxic activities. ► Candidates for treatment of both HBV and HBV-related HCC were first reported.