Table 2.
Inhibitory Activity and Selectivity of Coumarin Derivatives toward P450 1A2a
| Compoun d |
Short Name |
Structure | Ki (μM) | Selective Index (SI) |
|||
|---|---|---|---|---|---|---|---|
| 1A1 | 1A2 | 1B1 | 1A1/1A2 | 1B1/1A2 | |||
| 17 | 4P78PC |
|
25.2±2.6 | 1.29±0.33 | 5.04±0.76 | 20 | 3.9 |
| 18 | 3M4P78 PC |
|
18.4±0.4 | 1.72±0.27 | 21.2±2.3 | 11 | 12 |
| 19 | 4M78PC |
|
110±14 | 1.51±0.18 | 12.0±3.0 | 73 | 7.9 |
| 20 | 4TF78PC |
|
60.6±6.2 | 0.39±0.08 | 20.4±4.8 | 155 | 52 |
| 21 | 4P78FC |
|
12.0±0.3 | 5.02±0.16 | 4.62±0.78 | 2.4 | 0.9 |
| 22 | 3M4P78 FC |
|
11.6±0.4 | 3.70±0.73 | 22.6±6.1 | 3.1 | 6.1 |
| 23 | 4M78FC |
|
37.9±5.3 | 1.15±0.17 | 7.46±0.52 | 33 | 6.5 |
| 24 | 4TF78FC |
|
60.7±9.5 | 1.35±0.13 | 46.8±9.0 | 45 | 35 |
| 27 | 4M78Py C |
|
101±17 | 14.2±4.0 | 46.6±9.1 | 7.1 | 3.3 |
| 28 | 4P78DO C |
|
>200 | 3.55±0.84 | 30.1±4.6 | 56 | 8.5 |
a
The Ki values are represented as the mean ± SD μM of three independent experiments.