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. Author manuscript; available in PMC: 2022 Feb 1.
Published in final edited form as: Bioorg Med Chem. 2020 Dec 16;31:115952. doi: 10.1016/j.bmc.2020.115952

Table 1.

Anti-HBV activity and cytotoxicity of compounds 10a-i, 17a-f, 5 and 22.

Compound Anti-HBV activity (μM) Cytotoxicity CC50 (μM)
EC50 EC90 PBM CEM Vero HepG2a
4 1.2 ± 0.6 6.3 ± 2.9 69.1 3.7 14.7 27.0
10a 5.6 ± 1.60 >10 57.9 70.3 89.0 >100
10b 0.09 ± 0.07 3.05 ± 1.83 >100 >100 68.1 >100
10c 0.47 ± 0.53 4.10 ± 2.42 >100 >100 31.2 >100
10d 3.8 ± 3.1 9.67 ± 0.47 >100 >100 >100 >100
10e 1.1 ± 1.5 4.62 ± 4.50 >100 >100 41.9 93.9
10f 0.56 ± 0.69 2.95 ± 2.51 ≥100 37.9 80.1 >100
10g 0.08 ± 0.02 1.80 ± 1.23 >100 >100 13.4 >100
10h 0.41 ± 0.01 7.95 ± 0.07 >100 >100 62.4 >100
10i 5.16 ± 0.23 10.0 ± 0.03 >100 >100 91.4 >100
17a 0.004 ± 0.0001 0.06 ± 0.03 >100 14.6 >100 83.7
17b 0.005 ± 0.010 0.10 ± 0.04 ≥ 100 24.7 ≥ 100 95.4
17c 0.58 ± 0.08 5.64 ± 3.60 91.7 16.8 >100 89.9
17d 0.21 ± 0.74 3.44 ± 1.56 90.0 35.8 46.9 74.9
17e 0.16 ± 0.09 2.02 ± 1.68 >100 38.4 9.6 7.2
17f 0.01 ± 0.01 0.17 ± 0.23 >100 46.9 50.6 34.7
5 (GLP-26) 0.003 ± 0.002 0.014 ± 0.002 >100 >100 46.4 >100
22 0.006 ± 0.002 0.03 ± 0.003 >100 26.8 >100 83.9
GLS-4 0.08 ± 0.02 0.28 ± 0.06 28.4 68.7 17.7 >100
3TC 0.41 ± 0.36 1.65 ± 0.92 >100 >100 >100 >100
ETV 0.0006 ± 0.0003 0.011 ± 0.002 15.7 >100 >100 >100

ETV: Entecavir; 3TC: Lamivudine

b

AD38 cells are derived from HepG2 cells