Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue -, Pages 352-365Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.05.012
Keywords
Synthesis; Molecular hybrids; Caudatin derivatives; Anti-hepatitis B virus; Unique mechanisms
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Funding
- National Natural Science Foundation of China for Distinguished Young Scholars [81025023]
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Forty-six conjugated derivatives of caudatin with substituted cinnamic acids were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the derivatives exhibited potent anti-HBV activity, especially inhibiting the HBV DNA replication with the IC50 values from 2.44 to 22.89 mu M. Compound 18 showed significant activity against the secretion of HBsAg, HBeAg, and HBV DNA replication with IC50 values of 5.52, 5.52, 2.44 mu M, respectively, and had good safety (LD50 > 1250 mg/kg) according to the acute toxicity study. Preliminary mechanism investigation suggested that compound 18 exerted antivirus effects via interfering HBV X promoter and enhancer 1 to influence HBV transcriptions. (C) 2012 Elsevier Masson SAS. All rights reserved.
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