Inhibitory potency of 6,10-dimethoxy-2-arylbenzo[h]quinolin-4(1H)-ones 5a–j against CYP1B1, CYP1A1, and CYP1A2.
| ||||||
|---|---|---|---|---|---|---|
| Compound | R | IC50 values (nM) | IC50 ratio | |||
| 1B1 | 1A1 | 1A2 | 1A1/1B1 | 1A2/1B1 | ||
| 5a | H | 16.6 | 12.6 | 147.6 | 0.8 | 8.9 |
| 5b | o-F | 27.9 | 26.4 | 174 | 0.9 | 6.2 |
| 5c | m-F | 7.8 | 39.3 | 330.9 | 5.0 | 42.4 |
| 5d | m-Cl | 27.6 | 29.4 | 84.5 | 1.1 | 3.1 |
| 5e | m-Br | 3.6 | 19.8 | 587.6 | 5.5 | 163.2 |
| 5f | m-OCH3 | 7.1 | 35.8 | 190.1 | 5.0 | 26.8 |
| 5g | p-F | 3.9 | 10.5 | 2107 | 2.7 | 540.3 |
| 5h | p-OCH3 | 4.1 | 64.7 | >5000 | 15.8 | >1219.5 |
| 5i | p-CF3 | 34.4 | 300.4 | 1337 | 8.7 | 38.9 |
| 5j | 3,4,5-TriOCH3 | 163.9 | 809 | >5000 | 4.9 | >30.5 |