Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: A new class of hepatitis B virus inhibitors

A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC50 = 0.024 mM), HBV e antigen (IC50 = 0.028 mM) and remarkable selective indices (SIHBsAg > 108, SIHBeAg > 93), which was selected for further evaluation as a novel HBV inhibitor.

A series of alisol A derivatives were synthesized and assayed for their anti-HBV activities in vitro. The most active compound 6a showed IC50 of 0.024 and 0.028 mM to HBsAg and HBeAg, respectively, with CC50 > 2.6 mM, resulting remarkable selective indices (SIHBsAg > 108, SIHBeAg > 93).Figure optionsDownload as PowerPoint slide