Antiviral Library. HBV Subset. Focus on non-nucleoside compounds

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1 Antiviral Library BV ubset ocus on non-nucleoside compounds YAI, eb, 2015

2 Isosteric transformations eference Compounds examples W BV replication inhibition in immortalized murine hepatocyte (AML12)-derived stable cell line (AML12BV10) and liver ep DE19 cells (EC 50 < 1 M) in MTT assays. Baruch Blumberg Institute Me high diversity :C,, W spiro analogues BV replication inhibition in human hepatoma epg and epg2.117 cells (EC 50 <0.005 and M, respectively). It showed no cytotoxicity against epg2 cells (CC 50 >100 M upon 4 days incubation), in resazurin assays. Janssen &D Ireland C (2014) BV DA replication inhibition (98% at 500 nm) in human hepatoma epg cells in a qpc-based assay. EC Pharm W BV replication inhibition in human hepatoma epg (EC 50 < M) and epg2.117 (EC 50 = M) cells in in vitro assays without cytotoxicity against epg2 cells (CC 50 > 100 M) in resazurin assays Janssen &D Ireland Compound extracted from Lllicium henryi C (2014) everse transcriptase inhibitors inhibit IV-1 reverse transcriptase BV with an IC 50 =0.41 M (in human liver epg cancer cell) Peking University antiviral activity against BsAg and BeAg antigens (IC 50 = 0.43 and 0.5 M; in ELIA assays) and it also showed significant cytotoxicity (TC 50 = 3.28 M; using MTT method) in human hepatoma ep G cells with therapeutic index values of 7.6 and 6.6, respectively. Zhengzhou University C (2013) W :, BV replication inhibition EC 50 = 0.21 and 0.62 M, in epg and epg2.117 cells, respectively Antivir es 2014, 107: 6 BM601, a novel inhibitor of BV W C (2014) W significant antiviral activity against BsAg, BeAg antigens and inhibited BV DA replication (IC 50 =121.49, and mcm, respectively) in human hepatoma ep G cells without showing any significant cytotoxicity (CC50 = mcm) in MTT assays. Kunming Institute of Botany activity against human hepatoma ep G (stably transfected with BV genome) and ep G2.117 (stably inducible BV producing cell line) cells (EC 50 = and M, respectively). Janssen &D Ireland Me + W sanguinarine derivatives C (2014)

3 University of Maryland Bioorg Med Chem Lett 2005, 15(24): 5397 U compound inhibited BV-DA (IC 50 =5.4 M and CC 50 >100 M) U Toll-like receptor TL7 ligand that stimulated I-alpha production in human peripheral blood mononuclear cells (MEC = 0.03 M). eported to be useful for the treatment of BV al these compounds dose-dependently inhibit activity of BV polymerase (by 42% at 1 mcg/ml) and also CV A-dependent A-polymerase (5B, by 75% at 10 mcg/ml) in vitro W Gilead ciences W W (C)n antiviral activity in lymphoid MT2 cells infected with 92T599-MT2 IV-1 strain with and 80.45% inhibition at 1 and 0.1 M, respectively, and IC 50 values of and M, in p24 estimation assays. It also showed cell viabilities of and 89.93% at 1 and 0.1 mcm, respectively, against MT2 cells (CC 50 >1 M), in MTT cytotoxicity assays Bioorg Med Chem 2010, 18(14): 5048 n:1-3 W U CCC-0975, dose-dependently reduced cccda (10, 20 and 70% reduction at 1, 3 and 10 mcm, respectively) and DP-rcDA levels in epde19 cells. compound inhibited BV proliferation in epg2 cellular assays (EC 50 =0.01 M). IC 50 <1.1 µm and I>90.9 ch Pharm 2011, 344(2): 78 U Enanta Pharmaceuticals, Inc. W compound inhibited BV replication in human hepatoma cells with respective EC 50 and EC 90 values of 0.6 M and 3.4 M. 42nd Intersci Conf Antimicrob Agents Chemother (ICAAC) (eptember 27-30, an Diego) 2002, Abst C-04522, inhibited BV DA replication in epg cells with IC 50 and CC 50 values of 1.46 and M (I=151.06) respectively, in MTT assays C (2012) EC 50 =4 M,BV-transfected human ep G2 cells C (2012) J Med Chem 2011, 54(16): 5660

4 Topological analogues ChemDiv Compounds (examples) W C G J template W K G T T Et 2 Et Et C (2014) D D E C C (2014) K K C

5 Topological analogues ChemDiv Compounds (examples) template Me Antivir es 2014, 107: 6 W W K K K G P P V V V G J Me D

6 Topological analogues ChemDiv Compounds (examples) template Br D G Br C Me T D

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