Table 1.
Anti-HIV-1 activity and cytotoxicity of the novel phenylalanine derivatives in MT-4 cells infected with the HIV-1 NL4-3 virus.
 |
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|---|---|---|---|---|
| Compounds | R | EC50a (μM) | CC50b (μM) | SI |
| 13a |  |
8.00 ± 2.37 | > 20.68 | > 2.58 |
| 13b |  |
NAc | NAc | NDd |
| 13c |  |
NAc | NAc | NDd |
| 13d |  |
> 19.84 | > 19.84 | NDd |
| 13e |  |
NAc | NAc | NDd |
| 13f |  |
> 19.84 | > 19.84 | NDd |
| 13g |  |
> 21.53 | > 21.53 | NDd |
| 13h |  |
9.11 ± 2.88 | > 21.53 | > 2.36 |
| 13i |  |
8.98 ± 3.10 | > 21.53 | > 2.40 |
| 13j |  |
10.16 ± 2.22 | > 19.43 | > 1.91 |
| 13k |  |
NAc | NAc | NDd |
| 13l |  |
> 19.43 | > 19.43 | NDd |
| 13m |  |
4.33 ± 0.83 | > 57.74 | > 13.33 |
| 13n |  |
> 19.25 | > 19.25 | NDd |
| 13o |  |
14.93 ± 3.94 | > 20.02 | > 1.34 |
| 13p |  |
6.91 ± 2.43 | > 19.47 | > 2.82 |
| 13q |  |
NAc | NAc | NDd |
| 13r |  |
6.65 ± 1.47 | > 19.32 | > 2.91 |
| 13s |  |
NAc | > 18.74 | NDd |
| 13t |  |
10.45 ± 3.08 | > 16.56 | > 1.59 |
| PF-74 | - | 5.95 ± 1.32 | > 70.50 | > 11.85 |
a
EC50: the concentration of the compound required to achieve 50% protection of MT-4 cells against HIV-1-induced cytopathic effect, determined in at least triplicate against HIV-1 in MT-4 cells; values are the mean ± SD of at least two parallel tests.
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 MT-4 cells; values were averaged from at least four independent experiments.
C
NA: No anti-HIV-1 activity or cytotoxicity at the test concentration.
d
ND: Not determined.