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

Identifieur interne : 000E48 ( PubMed/Corpus ); précédent : 000E47; suivant : 000E49

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

Auteurs : Chang-An Geng ; Xiao-Yan Huang ; Yun-Bao Ma ; Xue-Mei Zhang ; Ji-Jun Chen

Source :

RBID : pubmed:25737009

English descriptors

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.

DOI: 10.1016/j.bmcl.2015.02.009
PubMed: 25737009

Links to Exploration step

pubmed:25737009

Le document en format XML

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