Table 2.
Sulfamoyl derivatives reduce HBV cccDNA formation in an HBeAg reporter cell-based assay.
| Compound | HBeAg Secretion | HBV DNA – Extracellular | HBV DNA – Intracellular | |||
|---|---|---|---|---|---|---|
|
| ||||||
| EC50 (μM) | EC90 (μM) | EC50 (μM) | EC90 (μM) | EC50 (μM) | EC90 (μM) | |
| 4a | 1.3 ± 0.4 | 4.6 ± 2.0 | 0.8 ± 0.2 | 7.8 ± 0.6 | 0.6 ± 0.002 | 4.3 ± 0.07 |
| 4f | 1.0 ± 0.05 | 3.2 ± 0.01 | 1.2 ± 0.6 | 6.3 ± 2.9 | 0.9 ± 0.05 | 9.7 ± 0.04 |
| 9 | 5.5 ± 0.02 | > 10 (61 ± 1.7) | 6.9 ± 0.1 | > 10 (76 ± 1.6) | 0.8 ± 0.01 | 8.1 ± 0.001 |
| 10 | 6.0 ± 2.9 | > 10 (66 ± 5.9) | 2.1 ± 1.3 | 9.5 ± 0.8 | 0.3 ± 0.04 | 3.6 ± 0.14 |
| 11 | 9.7 ± 2.5 | > 10 (67 ± 15.3) | 3.7 ± 0.1 | ≥ 10 (86 ± 2.1) | < 0.1 (63 ± 2.3) | 7.9 ± 0.17 |
| 3TC | > 10 (<1 ± 0.03) | N/A | 0.04 ± 0.03 | 0.3 ± 0.02 | < 0.01 (74 ± 4.4) | 0.7 ± 0.05 |
| ETV | > 10 (<1 ± 0.2) | N/A | 0.0007 ± 0.00001 | 0.1 ± 0.03 | ≤ 0.0001 (53 ± 0.5) | 0.009 ± 0.002 |
| GLS-4 | 0.7 ± 0.2 | 1.9 ± 0.04 | 0.2 ± 0.1 | 1.0 ± 0.1 | < 0.01 (82 ± 3.4) | 0.05 ± 0.0001 |
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.