期刊
ARCHIV DER PHARMAZIE
卷 341, 期 7, 页码 446-452出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.200800035
关键词
anti-HBV activities; 7-hydroxyquinoline-3-carboxylates; synthesis
Some new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives have been synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in HepG2.2.15 cells stable transfection with HBV. Compounds 13a, 11b, 11c, 12c, 13c, 11g, and 12g inhibited the expression of the viral antigens HBsAg or HBeAg in a low concentration, of which 11c (IC50 = 12.6 mu M, SI = 12.4), 12c (IC50 = 3.5 mu M, SI = 37.9), and 12g (IC50 = 2.6 mu M, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine (3TC, IC50 = 343.2 mu M, SI = 7.0).
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