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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 (IC 50 =0.024mM), HBV e antigen (IC 50 =0.028mM) and remarkable selective indices (SI HBsAg >108, SI HBeAg >93), which was selected for further evaluation as a novel HBV inhibitor.
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