Table 6. COX-1 and COX-2 Inhibitory Activities of Selected AKR1C3 Inhibitors; Data Derived from the Discontinuous Radioactive TLC Assay.
| compd | oCOX 1 IC50 (μM) | wt mCOX 2 IC50 (μM) | COX 1 IC50/COX 2 IC50 |
|---|---|---|---|
| indomethacin (1) | 0.05 | 0.20 | 0.25 |
| 8 | 0.49 | 0.09 | 5.44 |
| 20 | 15.27 (P)a | 3.27 (P) | 4.67 |
| 25 | 42.7% inhib. @ 25 μM | 35.6% inhib. @ 25 μM | n/a |
| 44 | 11% inhib. @ 25 μM | 17.6% inhib. @ 4 μM | n/a |
| 47 | 15.6% inhib. @ 25 μM (P) | 7.0 | n/a |
| 48 | 24.2% inhib. @ 25 μM (P) | 33.7% inhib. @ 25 μM (P) | n/a |
| 50 | 30.8% inhib. @ 25 μM (P) | 32.4% inhib. @ 25 μM (P) | n/a |
| 61 | 1.0 | 3.02 (P @ 61.4%) | 0.33 |
| 64 | 2.4 (P @ 56.1%) | 1.48 (P @ 62.6%) | 1.62 |
a
P = plateau; oCOX-1 = ovineCOX-1; mCOX-2 = murineCOX-2.