Table 2.
Anti-HIV-1 activity and cytotoxicity of Series II in TZM-bl cells infected with the HIV-1 NL4–3 virus.
 | |||||
|---|---|---|---|---|---|
| Compounds | R1 | R2 | EC50a(μM) | CC50b(μM) | SIc |
| 8a | H | - | 2.11±0.48 | >38.27 | >18.18 |
| 8b | CH3 | - | 5.96±2.05 | >37.27 | >6.25 |
| 8c | CH3O | - | 4.89±1.01 | >36.19 | >7.41 |
| 8d | - | F | 3.82±0.82 | >23.12 | >6.06 |
| 8e | - | Cl | 4.77±0.99 | >22.69 | >4.76 |
| 8f | - | Br | 5.62±1.84 | >21.60 | >3.85 |
| PF-74 | - | - | 0.52±0.18 | >47.00 | >90.91 |
a
EC50: the concentration of the compound required to achieve 50% protection of TZM-bl cells against HIV-1-induced cytopathic effect, determined in at least triplicate against HIV-1 in TZM-bl cells.
b
CC50: the concentration of the compound required to reduce the viability of uninfected cells by 50%, determined in at least triplicate against HIV-1 in TZM-bl cells; values were averaged from at least three independent experiments.
c
SI: selectivity index, the ratio of CC50/EC50.