Anti-HBV agents. Part 2: Synthesis and in vitro anti-hepatitis B virus activities of alisol A derivatives

作者：Zhang Quan; Jiang Zhi Yong^*; Luo Jie; Liu Ji Feng; Ma Yun Bao; Guo Rui Hua; Zhang Xue Mei; Zhou Jun; Chen Ji Jun

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(8): 2148-2153.

DOI：10.1016/j.bmcl.2009.02.122

• Anti-HBV activity
• Protostane-type triterpene
• Alisol A
• Derivatives
• Chemical modification

Chemical modi. cations 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 (IC(50) = 0.028 mM), HBeAg (IC(50) = 0.027 mM) and remarkable selective indices (SI(HBsAg) > 90, SI(HBeAg) > 93).

• 出版日期2009-4-15
• 单位中国科学院; 中国科学院昆明植物研究所