Anti-HBV agents. Part 2: Synthesis and in vitro anti-hepatitis B virus activities of alisol A derivatives |
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| Authors: | Quan Zhang Zhi-Yong Jiang Jie Luo Ji-Feng Liu Yun-Bao Ma Rui-Hua Guo Xue-Mei Zhang Jun Zhou Ji-Jun Chen |
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| Institution: | 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China;2. Graduate School of Chinese Academy of Sciences, Beijing 100039, PR China |
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| 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 = 0.028 mM), HBeAg (IC50 = 0.027 mM) and remarkable selective indices (SIHBsAg >90, SIHBeAg >93). |
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