Table 1.
IC50 values as determined in a radioactivity assay. All other compounds (meta-, para-, adamantyl series, benzyl and tert-butyl ester of indomethacin) were inactive in concentrations as high as 25 μM. Data are representative of an average of at least two independent experiments.
| Compound | IC50 [μM]
|
|
|---|---|---|
| COX-1 | COX-2 | |
| Indomethacin (1) | 0.027 | 0.127 |
| Indomethacin methyl ester (1i)39 | > 25 | 0.250 |
| Indoborin (4o) | > 25 | 3.680 |
| Indoborin methyl ester (1o) | 12.800 | 0.084 |
| Indoborin benzyl ester (2o) | 15.050 | 11.600 |
| Indoborin tert-butyl ester (1o) | > 25 | 1.410 |