Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors

  • Bioorg Med Chem Lett. 2015 Apr 1;25(7):1568-71. doi: 10.1016/j.bmcl.2015.02.009.
Chang-An Geng  1 ,  Xiao-Yan Huang  1 ,  Yun-Bao Ma  1 ,  Xue-Mei Zhang  1 ,  Ji-Jun Chen  2
Affiliations
  • 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
  • 2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China. Electronic address: [email protected].
PMID: 25737009 DOI: 10.1016/j.bmcl.2015.02.009
Abstract

Twenty-four derivatives of erythrocentaurin (ET) were synthesized and evaluated for their anti-HBV activities on HepG 2.2.15 cell line in vitro. Eight compounds 1, 2, 5, 8, 9, 1e, 1k, and 1m increased activity against HBV DNA replication with the SI values higher than 11. In particular, derivatives 1e and 1k exhibited the most potent inhibition on HBV DNA replication with the IC50 values of 0.026 mM (SI>70.8) and 0.045 mM (SI>36.0), respectively. The primary structure-activity relationships (SARs) of ET derivatives were summarized for exploring potent anti-HBV agents.

Keywords
Anti-HBV activity; Erythrocentaurin; Structure–activity relationships.
Products