Table 2.
Antiviral activity of novel compounds against highly DRV-resistant HIV-1 variants.
| Mean IC50 in nM (fold-change) | |||||
|---|---|---|---|---|---|
| LPV | 1 (DRV) | 5 | 6 | 21 (GRL-14213) | |
| cHIVLAIWT | 13 | 3.2 | 48.9 | 37.7 | 0.017 |
| HIVDRVRP20 | >1000 (>77) | 525.8 (164) | 219.3 (4) | 71.2 (2) | 0.0024 |
| HIVDRVRP30 | >1000 (>77) | 601 (187) | 946.4 (19) | 532.3 (14) | 0.14 |
| HIVDRVRP51 | >1000 (>77) | 5429.7 (1696) | >1000 | >1000 | 1.3 |
Numbers in parentheses represent fold changes in IC50s for each isolate compared to the IC50s for wild-type cHIVLAIWT. All assays were conducted in triplicate, and the data shown represent mean values (±1 standard deviation) derived from the results of three independent experiments. DRV, Darunavir; LPV, Lopinavir.