Table 3.
Inhibitory activity of NNRTIs and NRTIs against mutant HIV-1/IIIB strains in CEM cell cultures
| Compound | Fold increase of
EC50 versus wild-type virus
|
|||||
|---|---|---|---|---|---|---|
| Wild type* | 184-Ile | 184-Val | 188-His | 184-Ile + 188-His | 184-Val + 188-His | |
| Nevirapine | 1 (0.03) | 0.67 | 2.3 | 1.7 | 28 | 6.7 |
| BHAP U-90152 | 1 (0.006) | 1.0 | 0.50 | 10 | 167 | 83 |
| Pyridinone L-697661 | 1 (0.017) | 0.76 | 0.41 | — | 58 | 2.9 |
| TSAO-m3T | 1 (0.021) | 1.2 | 0.71 | 71 | 381 | 38 |
| 9-chloro-TIBO | 1 (0.02) | 1.0 | 0.50 | 45 | — | — |
| α-APA | 1 (0.005) | 2.8 | 0.80 | 100 | 960 | 70 |
| MKC-442 | 1 (0.002) | 1.0 | 1.0 | — | 390 | 25 |
| UC-10 | 1 (0.029) | 0.30 | 0.28 | 6.9 | 7.9 | 2.7 |
| UC-781 | 1 (0.002) | — | — | 8.0 | 37 | 8.0 |
| HBY 097 | 1 (0.001) | 1.0 | 3.0 | 2.0 | 19 | 5.0 |
| AZT | 1 (0.001) | 1.7 | 1.0 | 1.3 | 1.2 | 1.5 |
| ddI | 1 (0.92) | 2.8 | 2.6 | 0.49 | 1.3 | 1.3 |
| 3TC | 1 (0.01) | 70 | ≥5,000 | 0.60 | 280 | >2,000 |
*
Values in parentheses represent the 50% effective concentration (EC50) values of the drugs for wild-type HIV-1/IIIB (in μg/ml). ddI, dideoxyinosine.