Table 3. Biochemical Properties of 3-(2-Chloro or 2-Fluoropyridin-4-yl)-4-arylfuran-2(5H)-one Derivatives.
| no. | R1 | R2 | oCOX-1 IC50 (μM)a | mCOX-2 IC50 (μM)a |
|---|---|---|---|---|
| 41 | OCH3 | F | 4.60 | >25 |
| 42 | OCH3 | Cl | 4.40 | >25 |
| 43 | Cl | Cl | >25 | >25 |
| 44 | Cl | F | 15.70 | >25 |
| 45 | CH3 | Cl | 5.00 | >25 |
| 46 | CH3 | F | >25 | >25 |
| 47 | CN | F | 4.40 | >25 |
| 48 | CN | Cl | 3.00 | >25 |
a
IC50 values were determined by incubating several concentrations of inhibitors or DMSO vehicle with purified murine COX-2 (63 nM) or ovine COX-1 (22.5 nM) for 20 min followed by treatment with [1-14C]-AA (50 μM) at 37 °C for 30 s. Assays were run in duplicate.