Table 4.
Compounds | a HIV-1 RNase H (µM) | b HIV-1 IN LEDGF-Dependent (µM) |
---|---|---|
8 | >100 (100%) c | 0.33 ± 0.04 |
9 | >100 (100%) c | 0.11 ± 0.005 |
10 | >100 (100%) c | 1.76 ± 0.017 |
11 | >100 (100%) c | 0.024 ± 0.001 |
12 | >100 (100%) c | >100 (80%) c |
13 | >100 (92%) c | 5.96 ± 0.10 |
Raltegravir d | 0.058 ± 0.010 | |
RDS1759 d | 7.3 ± 0.10 |
a Compound concentration required to inhibit the HIV-1 RNase H activity by 50%. b Concentration required to inhibit the HIV-1 IN catalytic activities, in the presence of LEDGF, by 50%. c Percentage of control measured in the presence of 100 µM compound concentration. d Raltegravir and RDS1759 positive controls of IN LEDGF-dependent activity and RNase H function, respectively.