Table 2.
Anti-HIV-1 activity against mutant strains in MT-4 cells.
| Compd. | EC50a (nmol/L) |
||||||
|---|---|---|---|---|---|---|---|
| L100I | K103N | Y181C | Y188L | E138K | RES056b | F227L + V106Ab | |
| 5h | 8.2 ± 2.2 | 3.6 ± 0.9 | 9.2 ± 0.8 | 23 ± 6 | 6.5 ± 0.6 | 190 ± 50 | 930 ± 110 |
| 5j | 12 ± 2 | 3 ± 1 | 13 ± 2 | 17 ± 3 | 6.4 ± 0.1 | 34 ± 4 | 17 ± 4 |
| 6e | 22 ± 6 | 3.4 ± 0.5 | 11 ± 1 | 50 ± 8 | 5.3 ± 3.3 | 60 ± 7 | ≥16,410 |
| 6i | 29 ± 0.0 | 7.4 ± 2.1 | 17 ± 5 | 67 ± 16 | 10 ± 2 | 350 ± 80 | ≥3690 |
| 6k | 4.1 ± 0.5 | 2.3 ± 0.5 | 3 ± 0.2 | 10 ± 3 | 3.5 ± 0.8 | 60 ± 0.0 | 1040 |
| NVP | 460 ± 110 | 3190 ± 3900 | >4000 | >4000 | 57 ± 6 | >4000 | >4000 |
| EFV | 14 ± 0.0 | 30 ± 11 | 1.3 ± 0.1 | 82 ± 7 | 1.5 ± 0.1 | 71 ± 36 | 84 ± 20 |
| ETR | 4.7 ± 2.8 | 1.2 ± 0.1 | 6 ± 1.8 | 12 ± 0.0 | 5.4 ± 0.6 | 15 ± 6 | 10 ± 1 |
a
EC50: The effective concentration required to protect MT-4 cells against viral cytopathicity by 50%.
b
The double mutant strain (RES056 is referred to K103N/Y181C).