TABLE 1
Compounds tested for their effects on rat CYP2E1, CYP3A1/2, HO-1, and HO-2 enzyme activities
HO data for QC-15 have been reported previously by Kinobe et al. (2006). QC-xx synthesis and HO data for all other compounds have been reported previously by Vlahakis et al. (2009) and Roman et al. (2007, 2010). P450 data for QC-15, QC-47, and QC-121 have been reported previously by Vlahakis et al. (2009). They have been included for comparison and have been reproduced with permission. Data are represented as mean IC50 ± S.E.M. (μM).
| QC-xx | Structure | CYP2E1 | CYP3A1/2 | HO-1 | HO-2 | QC-xx | Structure | CYP2E1 | CYP3A1/2 | HO-1 | HO-2 |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 57 |  | 14.6 ± 2.9 | 5.1 ± 0.4 | 0.7 ± 0.4 | >100 | 15 |  | 20.8 ± 1.9 | 1.9 ± 0.1 | 4 ± 2 | >100 |
| 104 |  | >100 | 44.6 ± 6.0 | 14 ± 3 | >100 | 78 |  | 47 ± 6 | 1.18 ± 0.05 | 4 ± 1 | >100 |
| 143 |  | >100 | >100 | 39 ± 5 | >100 | 53 |  | 74 ± 2 | 33 ± 7 | 1.7 ± 0.7 | 10 ± 5 |
| 65 |  | 6.7 ± 0.2 | 53.7 ± 6.1 | 4 ± 2 | 11 ± 5 | 10 |  | 18 ± 3 | 12 ± 1 | 0.5 ± 0.1 | 4.0 ± 0.6 |
| 86 |  | >100 | Inactive | 2.6 ± 0.9 | 34 ± 3 | 79 |  | >100 | 8.1 ± 0.9 | 0.14 ± 0.06 | 2.6 ± 0.5 |
| 117 |  | Inactive | Inactive | 9.6 ± 0.2 | 37 ± 25 | 74 |  | >100 | 14 ± 2 | 0.06 ± 0.03 | 2 ± 1 |
| 118 |  | >100 | Inactive | 2.6 ± 0.9 | 20 ± 10 | 47 |  | 65.5 ± 15.2 | 3.9 ± 0.7 | 1.20 ± 0.01 | 4.4 ± 0.4 |
| 111 |  | Inactive | 28.4 ± 6.5 | 40 ± 2 | >100 | 121 |  | Inactive | 1.8 ± 0.2 | 0.9 ± 0.1 | 30 ± 4 |
| 124 |  | >100 | 88 ± 7 | 9 ± 2 | 145 ± 54 | 82 |  | >100 | 6 ± 2 | 3 ± 1 | >100 |