Table 1.
Anti-HBV activity and cytotoxicity
| Compound | Anti-HBV activity (μM)
|
Cytotoxicity CC50 (μM)
|
||||
|---|---|---|---|---|---|---|
| EC50 | EC90 | PBM | CEM | Vero | HepG2 | |
| 4a | 0.8 ± 0.2 | 7.8 ± 0.6 | 15.6 ± 0.01 | 14.0 ± 0.01 | 32.7 ± 0.11 | 37.1 ± 0.04 |
| 4b | 7.7 ± 1.6 | ≥ 10 (87 ± 0.2) | 25.8 ± 0.03 | 14.5 ± 0.07 | 18.3 ± 0.13 | 48.6 ± 0.01 |
| 4c | 4.5 ± 0.3 | 9.4 ± 0.1 | > 100 | 10.3 ± 0.09 | > 100 | > 100 |
| 4d | 6.7 ± 0.6 | > 10 (83 ± 1.7) | > 100 | 4.8 ± 0.78 | 21.3 ± 0.06 | > 100 |
| 4e | 9.2 ± 1.3 | > 10 (59 ± 14) | > 100 | ≤ 1 | 9.0 ± 0.02 | > 100 |
| 4f | 1.2 ± 0.6 | 6.3 ± 2.9 | 69.1 ± 0.07 | 3.7 ± 0.04 | 14.7 ± 0.04 | 27.0 ± 0.07 |
| 4g | > 10 | N/A | > 100 | 37.8 ± 0.16 | 39.6 ± 0.13 | >100 |
| 4h | 3.2 ± 0.4 | 8.9 ± 0.05 | 30.1 ± 0.06 | 13.6 ± 0.12 | 79.2 ± 0.03 | 62.3 ± 0.13 |
| 4i | 4.6 ± 1.2 | 10 ± 0.01 | > 100 | 22.9 ± 0.05 | 30.7 ± 0.02 | > 100 |
| 4j | 6.8 ± 0.9 | 9.6 ± 0.1 | > 100 | 3.8 ± 0.07 | 39.4 ± 0.26 | 88.2 ± 0.08 |
| 4k | 7.7 ± 2.5 | 9.3 ± 0.03 | > 100 | 3.6 ± 0.16 | 68.0 ± 0.03 | > 100 |
| 4l | > 10 | N/A | > 100 | 31.1 ± 0.16 | 13.1 ± 0.06 | 45.5 ± 0.11 |
| 4m | > 10 | N/A | > 100 | 31.6 ± 0.08 | > 100 | 76.8 ± 0.01 |
| 4n | > 10 | N/A | 58.1 ± 0.04 | 10.8 ± 0.05 | 39.1 ± 0.09 | > 100 |
| 4o | 2.7 ± 1.1 | > 10 (82 ± 3.2) | 13.0 ± 0.05 | 6.4 ± 0.04 | 5.8 ± 0.04 | 26.4 ± 0.03 |
| 4p | > 10 | N/A | > 100 | > 100 | > 100 | > 100 |
| 4q | > 10 | N/A | > 100 | > 100 | > 100 | > 100 |
| 4r | > 10 | N/A | > 100 | > 100 | > 100 | > 100 |
| 4s | > 10 | N/A | > 100 | > 100 | > 100 | > 100 |
| 9 | 6.9 ± 0.1 | > 10 (76 ± 1.6) | 39.2 ± 0.04 | 11.8 ± 0.12 | 30.7 ± 0.04 | 61.8 ± 0.03 |
| 10 | 2.1 ± 1.3 | 9.5 ± 0.8 | > 100 | 54.2 ± 0.11 | 29.1 ± 0.08 | > 100 |
| 11 | 3.7 ± 0.1 | ≥ 10 (86 ± 2.1) | > 100 | 74.5 ± 0.07 | 6.4 ± 0.06 | 80.4 ± 0.11 |
| 16 | ≥ 10 | N/A | 81.0 ± 0.01 | 13.6 ± 0.01 | 87.5 ± 0.01 | >100 |
| 19 | > 10 | N/A | > 100 | > 100 | 12.7 ± 0.03 | > 100 |
| 21 | > 10 | N/A | > 100 | 64.0 ± 0.04 | 84.3 ± 0.04 | > 100 |
| 32 | > 10 | N/A | > 100 | > 100 | > 100 | > 100 |
| 33 | > 10 | N/A | > 100 | 50.6 ± 0.10 | > 100 | > 100 |
| 34 | > 10 | N/A | 71.2 ± 0.03 | 36.0 ± 0.07 | > 100 | > 100 |
| 35 | > 10 | N/A | > 100 | > 100 | > 100 | > 100 |
| 3TC | 0.04 ± 0.03 | 0.3 ± 0.02 | > 100 | > 100 | > 100 | > 10 |
Data are the mean of replicates of two or three ± standard deviation (SD) from 2 independent experiments with representative results. N/A: not applied. Results in parenthesis: % of inhibition ± SD at 10 μM.