Synthesis and anti-hepatitis B virus evaluation of novel ethyl 6-hydroxyquinoline-3-carboxylates in vitro.
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.
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, Liaoning, PR China.
Yajing
Y
Liu
Yanfang
Y
Zhao
Xin
X
Zhai
Xusheng
X
Feng
Jinxin
J
Wang
Ping
P
Gong
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D006912:Hydroxyquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D006912:Hydroxyquinolines