Table 1.
Anti-HIV-1 activity and cytotoxicity of Series I in TZM-bl cells infected with the HIV-1 NL4–3 virus.
 | ||||
|---|---|---|---|---|
| Compounds | R | EC50a(μM) | CC50b(μM) | SIc |
| 6a | H | 6.23±1.20 | >41.53 | >6.67 |
| 6b | 4-F | 6.81±1.48 | >40.04 | >5.88 |
| 6c | 4-Cl | 9.88±3.30 | >38.76 | >3.92 |
| 6d | 4-Br | 8.21±2.50 | >35.69 | >4.35 |
| 6e | 2,4,6-tri(isopropyl) | 7.90±3.13 | >32.91 | >4.17 |
| 6f | 4-CH3O | 10.36±3.71 | >39.09 | >3.77 |
| 6g | 4-CH3 | 6.26±2.22 | >40.36 | >6.45 |
| 6h | 3,5-dimethyl | 9.22±3.53 | >39.25 | >4.26 |
| 6i | 2,4,6-trimethyl | 10.69±3.06 | >38.19 | >3.57 |
| 6j | 2-F | 10.81±2.20 | >40.04 | >3.70 |
| 6k | 3-F | 5.61±1.54 | >40.04 | >7.14 |
| 6l | 4-NO2 | >37.98 | >37.98 | - |
| 6m | 2-NO2 | 8.74±2.47 | >37.98 | >4.35 |
| 6n | 3-NO2 | 8.93±1.82 | >37.98 | >4.26 |
| 6o | 4-NH2 | 6.65±2.42 | >40.28 | >6.06 |
| 6p | 2-NH2 | 9.06±2.62 | >40.28 | >4.44 |
| 6q | 3-NH2 | 8.26±2.82 | >40.28 | >4.88 |
| 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.