Table 3.
Effects of twelve DGAT inhibitors on HCV genome replication. EC50 is an effective concentration required to inhibit 50% of HCV replication. CC50 is a cytotoxic concentration required to kill 50% of treated cells. Therapeutic index (TI) was calculated by dividing CC50 with EC50 values.
| Species | Code | EC50 (μM) | CC50 (μM) | TI |
|---|---|---|---|---|
| Benzimidazoles (pan DGATs inhibitors) | 10e | >10 | >10 | >1.0 |
| 10f | >10 | >10 | >1.0 | |
| 10h | 7.7 | >10 | >1.3 | |
| 10i | 0.9 | 3.9 | 4.4 | |
| 10j | 1.5 | 38.9 | 24.6 | |
| Indolyl hydrazides (DGAT-1 inhibitors) | 8h | 6.7 | >10 | >1.5 |
| 8i | 5.1 | >10 | >2.0 | |
| 8u | >10 | >10 | >1.0 | |
| Indolyl acrylamides (DGAT-2 inhibitors) | 5a | 1.9 | 3.7 | 1.9 |
| 5c | >10 | >10 | >1.0 | |
| 5h | 2.1 | 5.1 | 2.2 | |
| 5j | 1.1 | 3.4 | 3.0 | |
| DGAT-1 inhibitor | A922500 | 50.8 | 71.9 | 1.4 |