Article ID Journal Published Year Pages File Type
1376162 Bioorganic & Medicinal Chemistry Letters 2008 4 Pages PDF
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 (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.

Graphical abstractA 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 full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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