Table 1.
Compound | IC50 (nM)a against mPGES-1 | COX-1/2 Inhibition (%) at 100 µMb | ||
---|---|---|---|---|
ID | X | Human mPGES-1 | Mouse mPGES-1 | |
4a | H | 622 ± 121 | 7080 ± 627 | 0 ± 15 |
4b | Cl | 33 ± 3 | 157 ± 31 | 4.3 ± 6.0 |
4c | Br | 45 ± 8 | 917 ± 321 | 63 ± 0.8 |
4d | Me | 82 ± 10 | 18900 ± 4080 | 9.1 ± 6.6 |
4e | OH | 116 ± 17 | 2900 ± 293 | 68 ± 3.4 |
4f | OMe | 121 ± 20 | 146 ± 209 | 28 ± 3.6 |
4g | OEt | 186 ± 26 | 2410 ± 339 | 0 ± 15.1 |
4h | NO2 | 67 ± 20 | 698 ± 97 | 43 ± 3.2 |
4i | 87 ± 27 | 19100 ± 3490 | 56 ± 3.7 | |
6 | 69 ± 16 | 292 ± 47 | 17 ± 4.6 |
aData are expressed as the Mean ± SD of measurements in triplicate. bThe % inhibition of the compound at a concentration of 100 µM against the COX-1/2 (with equal amounts of COX-1 and COX-2 in terms of the enzyme activities).