Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 13, Pages 6522-6527Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.05.029
Keywords
hepatitis B virus; ethyl 6-hydroxyquinoline-3-carboxylates; synthesis; HepG2.2.15 cells
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A series of non-nucleoside ethyl 6-hydroxyquinoline-3-carboxylate derivatives were prepared and evaluated in HepG2.2.15 cells. Most compounds inhibited the expression of viral antigens HBsAg or HBeAg at low concentration. Six compounds, 9f(3), 12b(6), 12f(6), 13b(2), 13b(6), and 13f(6), displayed excellent intracellular inhibitory activity and selectivity towards the replication of HBV DNA. Of these six initial hits, compound 13b(6) was the most active. (c) 2008 Elsevier Ltd. All rights reserved.
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