Table 4.
analogue | 12-LOXb | 15-LOX-1b | 15-LOX-2b | 5-LOXb | COX−1/−2c | redox activityd |
---|---|---|---|---|---|---|
1 | 5.1 | >50 | >40 | >200 | NT | NT |
35 | 0.34 | 9.7 | >100 | >100 | NI | NI |
36 | 0.79 | >100 | >100 | >100 | NI | NI |
37 | 0.57 | >100 | >100 | >35 | NI | NT |
Selectivity profiling of 1, 35, 36, and 37.
IC50 values are reported in µM.
Compounds were tested at 15 µM and none of the compound exhibited inhibition above 10%.
UV–vis pseudoperoxidase activity assay was performed on 35 and 36, and no degradation of the hydroperoxide product was observed at 234 nm, indicating a nonreductive inhibitory mechanism; NI = no inhibition and NT = not tested.