Anti-HIV activity and cytotoxicity in MT-4 cells infected with HIV-1 IIIB and HIV-2 ROD.
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| Compounds | R1 | R2 | EC50a (μM) | CC50b (μM) | SIc | ||
| HIV-1 IIIB | HIV-2 ROD | HIV-1 IIIB | HIV-2 ROD | ||||
| Id-3a | H | H | 28 ± 7.8 | 3.6 ± 0.30 | >2.4 × 102 | >8.6 | >67 |
| Id-3b | H | 4-F | >77 | 11 ± 1.2 | 77 ± 28 | <1 | 7 |
| Id-3c | H | 3-F | 23 ± 4.8 | 4.6 ± 1.5 | >2.3 × 102 | >10 | >50 |
| Id-3d | H | 2-F | 24 ± 3.1 | 7.8 ± 2.0 | 1.4 × 102 ± 64 | 5.8 | 18 |
| Id-3e | H | 4-Cl | >8.9 | >9.0 | 9.0 ± 4.2 | <1 | <1 |
| Id-3f | H | 4-Br | >11 | >11 | 11 ± 2.9 | <1 | <1 |
| Id-3g | H | 4-CH3 | 33 ± 8.6 | 9.2 ± 1.1 | 64 ± 22 | 1.9 | 7.0 |
| Id-3h | H | 4-CH3O | 26 ± 4.1 | 21 ± 8.2 | 1.1 × 102 ± 34 | 4.2 | 5.2 |
| Id-3i | H | 4-CF3 | ≥37 | ≥41 | 42 ± 19 | ≤1.0 | ≤1.0 |
| Id-3j | H | 3-CF3 | >6.7 | >6.7 | 6.7 ± 3.3 | <1 | <1 |
| Id-3k | H | 2-CF3 | 21 ± 3.6 | 2.9 ± 1.8 | 1.3 × 102 ± 41 | 6.2 | 45 |
| Id-3l | H | 4-COOCH3 | >1.9 × 102 | 24 ± 6.2 | 2.0 × 102 ± 6.1 | <1 | 8.3 |
| Id-3m | H | 4-NO2 | >16 | >16 | 16 ± 6.3 | <1 | <1 |
| Id-3n | H | 3-NO2 | >24 | >24 | 24 ± 3.2 | <1 | <1 |
| Id-3o | H | 2-NO2 | 22 ± 4.3 | 2.5 ± 0.27 | 1.8 × 102 ± 14 | 8.2 | 72 |
| Id-3p | H | 4-NH2 | 21 ± 6.0 | 28 ± 4.1 | >2.3 × 102 | >11 | >8.2 |
| Id-3q | H | 3-NH2 | ≥2.0 × 102 | 27 ± 6.8 | >2.3 × 102 | ≤1 | >8.5 |
| Id-3r | H | 2-NH2 | 23 ± 5.7 | 5.4 ± 1.0 | 1.6 × 102± 38 | 7.0 | 30 |
| F-Id-3a | F | H | 25 ± 8.7 | 12 ± 4.0 | 1.1 × 102 ± 36 | 4.4 | 4.4 |
| F-Id-3b | F | 4-F | 20 ± 6.9 | 21 ± 13 | 77 ± 3.0 | 3.8 | 3.7 |
| F-Id-3c | F | 3-F | 25 ± 9.3 | 13 ± 6.6 | 99 ± 28 | 4.0 | 7.6 |
| F-Id-3d | F | 2-F | 22 ± 5.6 | 5.3 ± 1.4 | 1.4 × 102 ± 56 | 6.4 | 26 |
| F-Id-3e | F | 4-Cl | >19 | >19 | 19 ± 4.1 | <1 | <1 |
| F-Id-3f | F | 4-Br | >19 | >19 | 19 ± 6.0 | <1 | <1 |
| F-Id-3g | F | 4-CH3 | 32 ± 7.8 | 35 ± 3.0 | 74 ± 29 | 2.3 | 2.1 |
| F-Id-3h | F | 4-CH3O | 24 ± 3.4 | 31 ± 6.0 | 96 ± 32 | 4.0 | 3.1 |
| F-Id-3i | F | 4-CF3 | >18 | >18 | 18 ± 5.6 | <1 | <1 |
| F-Id-3j | F | 3-CF3 | >3.7 | >3.7 | 3.7 ± 1.4 | <1 | <1 |
| F-Id-3k | F | 2-CF3 | 12 ± 5.8 | 5.0 ± 0.81 | 1.1 × 102 ± 3.6 | 9.2 | 22 |
| F-Id-3l | F | 4-COOCH3 | 18 ± 3.5 | 26 ± 3.0 | 1.2 × 102 ± 55 | 6.7 | 4.6 |
| F-Id-3m | F | 4-NO2 | >18 | >18 | 18 ± 5.6 | <1 | <1 |
| F-Id-3n | F | 3-NO2 | 34 ± 5.0 | >47 | 47 ± 15 | 1.4 | <1 |
| F-Id-3o | F | 2-NO2 | 6.0 ± 2.4 | 6.3 ± 0.38 | 1.6 × 102 ± 45 | 27 | 25 |
| F-Id-3p | F | 4-NH2 | 18 ± 3.6 | 32 ± 5.6 | >2.2 × 102 | >12 | >6.9 |
| F-Id-3q | F | 3-NH2 | 23 ± 10 | 16 ± 2.1 | >2.2 × 102 | >10 | >14 |
| F-Id-3r | F | 2-NH2 | 18 ± 4.1 | 8.6 ± 0.77 | 1.6 × 102 ± 37 | 8.9 | 19 |
| PF74 | — | — | 0.75 ± 0.33 | 4.2 ± 2.0 | 32 ± 3.0 | 43 | 7.6 |
a
EC50: the concentration of the compound required to achieve 50% protection of MT-4 cells against HIV-induced cytotoxicity effect, determined in at least triplicate against HIV in MT-4 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 in MT-4 cells; values were averaged from at least three independent experiments.
c
SI: selectivity index, the ratio of CC50/EC50.