Table 1.
Anti-HIV-1 activity and cytotoxicity of the target compounds in TZM-bl cells infected with the HIV-1 NL4-3 virus.
 | ||||
|---|---|---|---|---|
| Compounds | R | EC50a(μM) | CC50b(μM) | SI |
| 5a | H | 3.92 ± 0.72 | >20.64 | >5.27 |
| 6a-1 |  |
3.99 ± 0.65 | >18.99 | >4.76 |
| 6a-2 |  |
3.74 ± 0.70 | >16.99 | >4.54 |
| 6a-3 |  |
>16.59 | >16.59 | |
| 6a-4 |  |
8.41 ± 2.42 | >16.16 | >1.92 |
| 6a-5 |  |
12.77 ± 2.91 | >16.16 | >1.27 |
| 6a-6 |  |
>16.16 | >16.16 | |
| 6a-7 |  |
>15.46 | >15.46 | |
| 6a-8 |  |
>16.30 | >16.30 | |
| 6a-9 |  |
3.13 ± 0.91 | >16.48 | >5.27 |
| 6a-10 |  |
3.30 ± 0.63 | >16.48 | >4.99 |
| 6a-11 |  |
3.46 ± 0.59 | >16.48 | >4.76 |
| 6a-12 |  |
>15.04 | >15.04 | |
| 5b | H | 3.30 ± 0.85 | >20.64 | >6.25 |
| 6b-1 |  |
14.81 ± 2.66 | >18.99 | >1.28 |
| 6b-2 |  |
12.74 ± 2.72 | >16.99 | >1.33 |
| 6b-3 |  |
>16.59 | >16.59 | |
| 6b-4 |  |
>16.16 | >16.16 | |
| 6b-5 |  |
>16.16 | >16.16 | |
| 6b-6 |  |
>16.16 | >16.16 | |
| 6b-7 | >15.46 | >15.46 | ||
| 6b-8 |  |
12.87 ± 3.10 | >16.30 | >1.27 |
| 6b-9 |  |
13.52 ± 2.47 | >16.48 | >1.22 |
| 6b-10 |  |
9.56 ± 2.31 | >16.48 | >1.72 |
| 6b-11 |  |
>16.48 | >16.48 | |
| 6b-12 |  |
>15.04 | >15.04 | |
| 5c | H | 13.62 ± 2.68 | >20.63 | >1.51 |
| 6c-1 |  |
>18.99 | >18.99 | |
| 6c-2 |  |
12.91 ± 2.89 | >16.99 | >1.32 |
| 6c-3 |  |
>16.59 | >16.59 | |
| 6c-4 |  |
>16.16 | >16.16 | |
| 6c-5 |  |
>16.16 | >16.16 | |
| 6c-6 |  |
>16.16 | >16.16 | |
| 6c-7 |  |
>15.46 | >15.46 | |
| 6c-8 |  |
12.38 ± 2.28 | >16.30 | >1.32 |
| 6c-9 |  |
11.87 ± 3.13 | >16.48 | >1.39 |
| 6c-10 |  |
12.69 ± 3.46 | >16.48 | >1.30 |
| 6c-11 |  |
13.02 ± 2.97 | >16.48 | >1.27 |
| 6c-12 |  |
12.19 ± 2.56 | >15.04 | >1.23 |
| PF-74 | 0.28 ± 0.06 | >23.50 | >83.93 | |
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.