Table 1.
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
AD38 cells are derived from HepG2 cells