Synthesis and anti-HBV activities evaluation of new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives in vitro.
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 (IC(50 )= 12.6 microM, SI = 12.4), 12c (IC(50 )= 3.5 microM, SI = 37.9), and 12g (IC(50) = 2.6 microM, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine (3TC, IC(50) = 343.2 microM, SI = 7.0).
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.
Yajing
Y
Liu
Yanfang
Y
Zhao
Xin
X
Zhai
Xiuping
X
Liu
Lixue
L
Sun
Yanxia
Y
Ren
Ping
P
Gong
D000998:Antiviral Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D002264:Carboxylic Acids / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D005786:Gene Expression Regulation / Q000187:drug effects; D006514:Hepatitis B Surface Antigens / Q000187:drug effects; D006513:Hepatitis B e Antigens / Q000187:drug effects; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D006912:Hydroxyquinolines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D019259:Lamivudine / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014162:Transfection
D000998:Antiviral Agents; D002264:Carboxylic Acids; D006514:Hepatitis B Surface Antigens; D006513:Hepatitis B e Antigens; D006912:Hydroxyquinolines; D019259:Lamivudine