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  • Title: Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors.
    Author: Zhang Q, Jiang ZY, Luo J, Cheng P, Ma YB, Zhang XM, Zhang FX, Zhou J, Chen JJ.
    Journal: Bioorg Med Chem Lett; 2008 Aug 15; 18(16):4647-50. PubMed ID: 18644720.
    Abstract:
    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)=0.024 mM), HBV e antigen (IC(50)=0.028 mM) 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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