Table 1.
Inhibition of HIV-1 integrase enzymatic activity.
| Compound | IN enzymatic activity (IC50-µM) | |
|---|---|---|
| a Overall | b ST | |
| 7a | 1.74 ± 1.32 | 1.07 ± 0.76 |
| 7b | 0.42 ± 0.29 | 1.36 ± 0.64 |
| 7c | 5.76 ± 1.82 | 8.84 ± 5.60 |
| 7d | 2.61 ± 1.17 | 6.79 ± 0.64 |
| 7e | 51.76 ± 33.81 | 55.85 ± 43.83 |
| 7f | 3.83 ± 2.21 | 9.47 ± 1.06 |
| 7g | 7.34 ± 1.32 | 23.54 ± 17.78 |
| 7h | 7.69 ± 5.59 | 5.49 ± 2.67 |
| 7i | 2.17 ± 1.65 | 5.24 ± 1.34 |
| CHI-1043 | 0.08 ± 0.003 | 0.14 ± 0.11 |
a Concentration required to inhibit the in vitro overall integrase activity by 50%; b Concentration required to inhibit the in vitro strand transfer step by 50%.