Abstract:
:A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC(50) = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC(50) = 0.026 mM, SI > 51) and the replication of HBV DNA (IC(50) = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Guo RH,Zhang Q,Ma YB,Luo J,Geng CA,Wang LJ,Zhang XM,Zhou J,Jiang ZY,Chen JJdoi
10.1016/j.ejmech.2010.11.019subject
Has Abstractpub_date
2011-01-01 00:00:00pages
307-19issue
1eissn
0223-5234issn
1768-3254pii
S0223-5234(10)00814-7journal_volume
46pub_type
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