Table 2.
Effect of 9a–9o on HIV-1 mutants.
| Compd. | EC50 (nmol/L)a |
||||
|---|---|---|---|---|---|
| L100I | K103N | Y181C | Y188L | E138K | |
| 9a | 6.3 ± 0.3 | 3.2 ± 0.7 | 16.1 ± 2.3 | 33.0 ± 4.0 | 6.5 ± 0.5 |
| 9b | 18.1 ± 3.4 | 2.9 ± 0.1 | 11.0 ± 0.3 | 144 ± 25.9 | 3.6 ± 0.7 |
| 9c | 20.5 ± 1.3 | 6.5 ± 0.2 | 27.6 ± 3.0 | 137 ± 8.1 | 19.4 ± 4.8 |
| 9d | 117 ± 17.7 | 14.4 ± 1.5 | 901 ± 208 | 41,793 ± 509 | 34.9 ± 3.2 |
| 9e | 18.5 ± 3.6 | 3.8 ± 0.2 | 22.5 ± 3.5 | 564 ± 97.0 | 11.0 ± 2.1 |
| 9f | 11.1 ± 0.5 | 3.2 ± 0.6 | 29.9 ± 1.9 | 85.3 ± 8.4 | 7.9 ± 0.2 |
| 9g | 8.2 ± 1.4 | 1.9 ± 0.2 | 15.4 ± 1.0 | 161 ± 27.6 | 3.5 ± 0.8 |
| 9h | 323 ± 44.5 | 20.1 ± 3.0 | 274 ± 7.7 | 1584 ± 103.2 | 38.9 ± 4.1 |
| 9i | 560 ± 137 | 95.6 ± 17.6 | 383 ± 15.0 | 1753 ± 122.6 | 217 ± 18.4 |
| 9j | 327 ± 44.9 | 35.1 ± 8.1 | 350 ± 21.2 | >48,410 | 42.4 ± 6.7 |
| 9k | 327 ± 54.8 | 35.4 ± 12.3 | 355 ± 12.6 | 42,967 ± 532 | 45.9 ± 5.9 |
| 9l | 22.2 ± 6.2 | 3.0 ± 0.3 | 50.7 ± 3.8 | 720 ± 272 | 13.6 ± 1.2 |
| 9m | 13704 ± 1137 | 1691 ± 165 | 46,560 ± 1255 | >178,250 | 2492 ± 388 |
| 9n | 1996 ± 275 | 396 ± 42.1 | 6148 ± 316 | >13,450 | 490 ± 54.2 |
| 9o | 2658 ± 252 | 399 ± 30.7 | 2689 ± 255 | 151,258 ± 48,209 | 396 ± 17.1 |
| NVP | 2100 ± 750 | >10,080 | >15,870 | >15,870 | 2100 ± 30 |
| EFV | 440 ± 70 | 102 ± 50. | 7 ± 0.0 | 290 ± 40 | 6 ± 0.0 |
| ETR | 7 ± 0.0 | 3 ± 0.0 | 12 ± 10 | 20 ± 10 | 7 ± 10 |
a
EC50: The effective concentration required to protect MT-4 cells against viral cytopathicity by 50%, and values were averaged from at least three independent experiments.