In vitro COXs suppression, IC50 and SI values of the selected derivatives (reproduced with permission from G. N. Tageldin, et al., Bioorg. Chem., 2018, 78, 358–371, © 2018 Elsevier)78.
| Tested compound | COX-1, IC50 (μM)a | COX-2, IC50 (μM) | SIb (COX-1/COX-2) |
|---|---|---|---|
| 10 | 2.74 | 0.22 | 12.45 |
| 11 | 5.88 | 0.69 | 8.52 |
| 12 | 3.89 | 0.54 | 7.20 |
| 13 | 4.74 | 0.69 | 6.86 |
| 14 | 4.74 | 0.87 | 5.44 |
| Celecoxib | 5.46 | 0.78 | 7.23 |
| Diclofenac sodium | 6.74 | 1.10 | 6.12 |
Values are average of three readings obtained and the variation from the average is ±10% of the average value.
In vitro COX-2 selectivity indices (COX-1 IC50/COX-2 IC50).