Table 3.
Inhibitory activity of the target compounds against WT HIV-1 RT.a
| Compd. | RT IC50b (μg/mL) | RNase H IC50d (μg/mL) | Compd. | IC50 (μg/mL) | RNase H IC50 (μg/mL) |
|---|---|---|---|---|---|
| 5a | 0.047 ± 0.003 | >600 | 6d | 0.128 ± 0.007 | >600 |
| 5b | 0.136 ± 0.011 | >600 | 6e | 0.055 ± 0.003 | >600 |
| 5c | 0.112 ± 0.003 | >600 | 6f | 0.138 ± 0.131 | >600 |
| 5d | 0.149 ± 0.004 | >600 | 6g | 0.069 ± 0.002 | >600 |
| 5e | 0.098 ± 0.004 | 332 ± 60 | 6h | 0.171 ± 0.018 | >600 |
| 5f | 0.242 ± 0.020 | >600 | 6i | 0.117 ± 0.012 | >600 |
| 5g | 0.145 ± 0.009 | >600 | 6j | 0.081 ± 0.003 | >600 |
| 5h | 0.081 ± 0.003 | >417 | 6k | 0.052 ± 0.012 | >600 |
| 5i | 0.146 ± 0.016 | 259 ± 20 | 6l | 0.115 ± 0.021 | >600 |
| 5j | 0.096 ± 0.016 | >600 | 6m | 0.096 ± 0.013 | >543 |
| 5k | 0.368 ± 0.021 | >600 | 6n | 0.087 ± 0.008 | >600 |
| 6a | 0.035 ± 0.008 | >600 | NVP | 0.102 ± 0.026 | ND |
| 6b | 0.033 ± 0.004 | >600 | EFV | 0.0014 ± 0.0004 | ND |
| 6c | 0.127 ± 0.026 | >600 | ETRc | 0.100 ± 0.000 | ND |
| SGI/DS8000e | – | 1.4 ± 0.1 |
–Not applicable.
a
Data represent the mean values of at least two separate experiments.
b
IC50: inhibitory concentration of test compound required to inhibit biotin deoxyuridine triphosphate (biotin-dUTP) incorporation into WT HIV-1 RT by 50%.
c
The data were obtained from the same laboratory with the same method.
d
Data represent the mean values of four times of separate experiments.
e
Reference compound for HIV-1 RT RNase H inhibitory activity.