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In vitro COX-1/COX-2 inhibition (IC50, μmol/L) and selectivity index for compounds 4–8, and standard agent.
| Compd. | COX-1a | COX-2a | COX-2 selectivityb |
|---|---|---|---|
| 4 | 0.5 | 0.0011 | 455 |
| 5 | 96.57 | 0.0092 | 10,479 |
| 6 | >100.00 | 0.092 | >1087 |
| 7 | >100.00 | 0.53 | >189 |
| 8 | >100.00 | <0.01 | ‒ |
| Celecoxib | >100.00 | 0.056 | 295 |
The result (IC50, μmol/L) is the mean of three determinations acquired using a COX fluorescent inhibitor screening assay kit (Cayman Chemical, MI, USA).
COX-2 selectivity index (COX-1 IC50/COX-2 IC50).
