Table 1. SAR Studies on the COXs Inhibition by 1a−d (n = 3).
| COX-1 |
COX-2 |
|||
|---|---|---|---|---|
| compound | ihibition (100 μM, %) | IC50 (μM) | ihibition (100 μM, %) | IC50 (μM) |
| 1a (synthesized) | 81 ± 11 | 0.01 | 89 ± 0.7 | 18 |
| 1ba | 79 ± 6.4 | 0.01 | 76 ± 1.4 | 39 |
| 1c | <0 | >400 | 14 ± 0.9 | >400 |
| 1d | <0 | >400 | 13 ± 2.0 | >400 |
| 1a (purchased) | 110 ± 11 | 0.12 | 83 ± 0.45 | 20 |
| aspirin | 38 ± 3.1 | >100 | 2 ± 1.5 | >400 |
These data are in accord with those reported previously.20