IC50 values and lipophilicities of the 4-substituted 7-methoxy coumarins
| Compound | IC50 Value | Σf |
|---|---|---|
| μM | ||
| MAMC | 132 ± 19 | 0.392 |
| MMAMC | 90 ± 9 | 0.642 |
| EMAMC | 26 ± 3 | 1.161 |
| PMAMC | 2.0 ± 0.1 | 1.680 |
| BMAMC | 0.51 ± 0.03 | 2.199 |
| DiMMAMC | 171 ± 16 | 1.106 |
| MMPyrC | 138 ± 23 | N.D. |
The IC50 measurements were performed with CYP2D6 expressed in human lymphoblasts, and dextromethorphan as reference compound. Values are the mean ± S.D. (n = 3). Lipophilicities (Σf) were calculated according to the hydrophobic fragmental constant approach by Rekker and Mannhold (1992). Because the fragmental constant of the pyridine structure was not available, the lipophilicity of MMPyrC could not be determined.
N.D., not determined.