Table 1.
Antiviral activity of compounds against wt NL4-3 and NNRTI-resistant HIV-1 strains.
| HIV-1 wt MT EC50 1 (µM) |
HIV-1 K103N-Y181C MT4 EC50 1 (µM) |
MT4 CC50 2 (µM) |
SI 3 | |
|---|---|---|---|---|
| 13 | 10.1 ± 4.7 | 12.4 ± 0.8 | 61.5 ± 2.2 | 6.1 |
| 21 | 5.0 ± 1.4 | 8.7 ± 0.1 | 31.8 ± 0.4 | 6.4 |
| RDS1759 | 8.2 ± 0.9 | 4.6 ± 1.1 | 39 ± 4.4 | 4.7 |
| AZT | 0.007 ± 0.005 | 0.0031 ± 0.0007 | >3.7 | >500 |
| EFV | 0.050 ± 0.012 | >1.58 | >0.31 | >6.25 |
| NVP | 0.67 ± 0.22 | >3.7 | >3.7 | >5.5 |
| RAL | 0.0022 ± 0.0001 | 0.004 ± 0.001 | >2.25 | >1987 |
1 EC50: effective concentration 50 or concentration of compound required to inhibit 50% of HIV-induced cell death, evaluated with the MTT method in MT4 cells; 2 CC50: cytotoxic concentration 50 or concentration of compound required to induce 50% of death of non-infected cells, evaluated with the MTT method in MT4 cells; 3 SI: selectivity index, indicates the ratio between the CC50 and the EC50; AZT: azidothymidine, EFV: efavirenz, NVP: nevirapine, RAL: raltegravir; Data represent mean and SD of three independent experiments.