Table 3.
HIV neutralization activity of trisulfonaphthyl moleculesa
 | |||||||
|---|---|---|---|---|---|---|---|
| Compound | R1 | R2 | IC50 (μM) | ||||
| YU2 | JRCSF | 89.6 | HxB2 | NL4–3 | |||
| 11a | Me |  |
53.8 | 22.1 | 9.2 | 8.1 | 7.0 |
| 11b | Me | CF3 | NAb | 83.3 | 79.7 | NA | 80.1 |
| 11c | Me | Ph | 137.4 | 64.8 | 100.9 | 51.1 | 33.1 |
| 11d | Ph |  |
24.7 | 10.2 | 3.2 | 7.5 | 5.8 |
| 11e | Ph | CF3 | 27.9 | 5.8 | 2.4 | 6.8 | 6.3 |
| 11f | Ph | Ph | 43.7 | 30.7 | 8.4 | 3.6 | 7.1 |
| 11g | Ph |  |
30.7 | 9.9 | 2.9 | 2.5 | 3.6 |
| 11h |  |
 |
74.9 | 36.2 | 22.3 | 10.1 | 15.6 |
| 11i | Ph |  |
22.3 | 14.9 | 8.9 | 5.2 | 7.7 |
| 11j | Ph |  |
23.8 | 8.0 | 3.8 | 1.1 | 2.9 |
| 11k | Ph |  |
30.9 | 19.5 | 6.7 | 12.0 | 10.2 |
| 11l | Ph |  |
52.8 | 29.8 | 14.8 | 14.2 | 10.7 |
| 11m | CF3 |  |
297.7 | NAb | NA | 80.0 | 103.7 |
| 11n |  |
 |
62.4 | 24.1 | 14.6 | 9.4 | 11.2 |
a
HIV-1 strains include CCR5-tropic strains YU2 and JRCSF, dual CXCR4/CCR5-tropic strain 89.6 and CXCR4-tropic strain HxB2.
b
NA, not active at concentrations as high as 400 μM.