2. Academic Validation
  3. Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors

Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors

  • Bioorg Med Chem Lett. 2008 Aug 15;18(16):4647-50. doi: 10.1016/j.bmcl.2008.07.012.
Quan Zhang 1,  Zhi-Yong Jiang,  Jie Luo,  Pi Cheng,  Yun-Bao Ma,  Xue-Mei Zhang,  Feng-Xue Zhang,  Jun Zhou,  Ji-Jun Chen
Affiliations

Affiliation

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Lanhei Road, Kunming 650204, PR China.
PMID: 18644720 DOI: 10.1016/j.bmcl.2008.07.012
Abstract

A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC(50)=0.024 mM), HBV e antigen (IC(50)=0.028 mM) and remarkable selective indices (SI(HBsAg)>108, SI(HBeAg)>93), which was selected for further evaluation as a novel HBV Inhibitor.

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