Inhibitory potency of 3-hydroxy-2-arylbenzo[h]quinolin-4(1H)-ones 3a–d, 2-arylbenzo[h]quinolin-4(1H)-one 3eand its chemical isomers 4a,b against CYP1B1, CYP1A1, and CYP1A2.
| |||||||
|---|---|---|---|---|---|---|---|
| Compound | R1 | R | IC50 values (nM) | IC50 ratio | |||
| 1B1 | 1A1 | 1A2 | 1A1/1B1 | 1A2/1B1 | |||
| 3a | OH | H | 86.7 | 897.7 | >5000 | 10.4 | >57.7 |
| 3b | OH | o-F | 85.9 | 1783 | >5000 | 20.8 | >58.2 |
| 3c | OH | p-OH | 141.7 | 525.1 | >5000 | 3.7 | >35.3 |
| 3d | OH | p-F | 93.3 | 333.5 | >5000 | 3.6 | >53.6 |
| 3e | H | H | 17.3 | 103.2 | 483.5 | 6.0 | 27.9 |
| 4a | OH | — | 7.6 | 18.5 | 146.9 | 2.4 | 19.3 |
| 4b | OCH3 | — | NIa | NI | NI | — | — |
NI = no inhibition.