Synthesis and in vitro anti-hepatitis B virus activities of some ethyl 5-hydroxy-1H-indole-3-carboxylates.
A series of ethyl 5-hydroxy-1H-indole-3-carboxylates 6A-10T were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC50 and selective index of inhibition on replication of HBV DNA of compounds 10(L) (1.52 microg/ml, 9.38) and 10(P) (2.00 microg/ml, 8.85) were higher than those of the other evaluated compounds including lamivudine (7.02). Compounds 7E and 10J exhibited significant anti-HBV activities, and the IC50 values on replication of HBV DNA of these compounds were 24.90 and 15.41 microg/ml, respectively, which were far more potent than the positive control lamivudine 228.00 microg/ml.
Zhao
Chunshen
C
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Zhao
Yanfang
Y
Chai
Huifang
H
Gong
Ping
P
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D004261:DNA Replication / Q000187:drug effects; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization
D000998:Antiviral Agents; D007211:Indoles