Table 1.
Antiviral activity of GRL-04810 and GRL-05010 against HIV-1LAI and their cytotoxicitiesa
| Compound | EC50 (μM) | CC50 (μM) | Selectivity indexb |
|---|---|---|---|
| SQV | 0.021 ± 0.001 | 17.7 ± 3.4 | 843 |
| LPV | 0.020 ± 0.001 | 26.8 ± 0.9 | 1,340 |
| ATV | 0.005 ± 0.001 | 28.6 ± 0.9 | 5,720 |
| APV | 0.03 ± 0.001 | >100 | >3,333 |
| DRV | 0.005 ± 0.001 | >100 | >20,000 |
| GRL-04810 | 0.0008 ± 0.0002 | 17.5 ± 0.9 | 21,875 |
| GRL-05010 | 0.003 ± 0.001 | 37.0 ± 0.4 | 12,333 |
a
MT-2 cells (104/ml) were exposed to 100 TCID50 of HIV-1LAI and cultured in the presence of various concentrations of each PI, and the EC50s were determined by MTT assay. All assays were conducted in duplicate, and the data shown represent mean values derived from the results of three independent experiments.
b
Each selectivity index denotes a ratio of the CC50 to EC50 against HIV-1LAI.