Table 1.
Inhibitory activity of bis-arylsulfonamides and aryl sulfonimides against PAI-1 and ATIII.
| Cmpd | Structure | PAI-1 Inhibition IC50, μMa | ATIII Inhibition IC50, μMa |
|---|---|---|---|
| 2b |  |
>300 | >300 |
| 3a |  |
518 (±64) |
>3000b |
| 3b |  |
9.32 (±0.36) |
>1000b |
| 3c |  |
>3000 | >3000 |
| 3d |  |
1384 (±112) |
>3000 |
| 4 |  |
>300c | >300 |
| 5 |  |
343 (±14) |
>1000 |
| 6 |  |
>300 | >300 |
| 7 |  |
>300c | >300 |
| 8 |  |
>300 | >300 |
| 13 |  |
128 (±18) |
>3000 |
| 17a |  |
2.67 (±0.27) |
>1000 |
| 17b |  |
0.284 (±0.016) |
>300b |
| 17c |  |
4.82 (±0.32) |
>300 |
| 17d |  |
0.594 (±0.086) |
>300 |
a
Each value is the average of at least 3 determinations; standard error is given in parentheses.
b
<30% of ATIII was inhibited at the highest compound concentration used.
c
<30% of PAI-1 was inhibited at the highest compound concentration used.