Table 1. Biochemical properties of fluorinated indomethacin and celecoxib derivatives.
Compound No. | Structure | Purified Enzyme IC50 (μM) | RAW246.7 Cellsa IC50 (μM) COX-2 | |
---|---|---|---|---|
COX-1 | COX-2 | |||
1 | > 4 | 0.14 | 0.68 | |
2 | > 4 | 0.09 | 0.01 | |
3 | > 4 | 0.26 | 0.16 | |
4 | > 4 | 0.10 | 0.04 | |
5 | > 4 | 0.16 | 0.24 | |
6 | > 4 | 0.13 | 0.11 | |
7 | > 4 | 0.16 | 0.08 | |
8 | > 4 | 0.60 | N.T. | |
9 | > 4 | 1.95 | N.T. | |
10 | > 4 | 3.40 | N.T. | |
11 | > 4 | 1.3 | N.T. | |
Indomethacin | 0.05 | 0.75 | 0.01 | |
Celecoxib | > 4 | 0.03 | N.T. |
Assays were conducted as described in Materials and Methods. Compounds that are poor inhibitors of COX-2 in the purified enzyme assay were not tested (N.T.) in intact cells.