1. Anti-HBV agents. Part 2: Synthesis and in vitro anti-hepatitis B virus activities of alisol A derivatives
- Author
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Zhang, Quan, Jiang, Zhi-Yong, Luo, Jie, Liu, Ji-Feng, Ma, Yun-Bao, Guo, Rui-Hua, Zhang, Xue-Mei, Zhou, Jun, and Chen, Ji-Jun
- Subjects
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ANTIVIRAL agents , *HEPATITIS B virus , *STRUCTURE-activity relationship in pharmacology , *CELL-mediated cytotoxicity , *DRUG activation , *CELL surface antigens - Abstract
Abstract: Chemical modifications were performed on hydroxyl groups at C-11,23,24,25 positions and C-13(17) double bond of alisol A for structure–activity relationship study. Forty-one derivatives of alisol A were synthesized and assayed for their in vitro anti-hepatitis B virus (HBV) activities and cytotoxicities. Of them, 14 compounds were active against HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion in HepG 2.2.15 cells, and the most promising compound 25 exhibited high activities against secretion of HBsAg (IC50 =0.028mM), HBeAg (IC50 =0.027mM) and remarkable selective indices (SIHBsAg >90, SIHBeAg >93). [Copyright &y& Elsevier]
- Published
- 2009
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