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

  • Bioorg Med Chem Lett. 2009 Apr 15;19(8):2148-53. doi: 10.1016/j.bmcl.2009.02.122.
Quan Zhang  1 ,  Zhi-Yong Jiang ,  Jie Luo ,  Ji-Feng Liu ,  Yun-Bao Ma ,  Rui-Hua Guo ,  Xue-Mei Zhang ,  Jun Zhou ,  Ji-Jun Chen
Affiliations
  • 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, PR China.
PMID: 19289281 DOI: 10.1016/j.bmcl.2009.02.122
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 (IC(50)=0.028 mM), HBeAg (IC(50)=0.027 mM) and remarkable selective indices (SI(HBsAg) >90, SI(HBeAg) >93).