Anti-HBV agents. Part 2: Synthesis and in vitro anti-hepatitis B virus activities of alisol A derivatives
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- 作者：Quan Zhang ; Zhi-Yong Jiang ; Jie Luo ; Ji-Feng Liu ; Yun-Bao Ma ; Rui-Hua Guo ; Xue-Mei Zhang ; Jun Zhou ; Ji-Jun Chen
- 关键词：Anti-HBV activity ; Protostane-type triterpene ; Alisol A ; Derivatives ; Chemical modification
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 April 2009
- 年：2009
- 卷：19
- 期：8
- 页码：2148-2153
- 全文大小：2279 K
文摘
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 = 0.028 mM), HBeAg (IC50 = 0.027 mM) and remarkable selective indices (SIHBsAg >90, SIHBeAg >93).