Table 1.
Inhibitory potencies and selectivity indices (SI) of stilbene derivatives.
| Compounds | IC50 CYP1B1 (μM)b | PI | IC50 CYP1A1 (μM)b | IC50 CYP19A1 (μM)c | IC50 phLM (μM)d | SI (1B1:1A1) | SI (1B1:19A1) | SI (1B1:phLM) | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Dark | Lighta | Dark | Lighta | Dark | Lighta | Dark | Lighta | |||||
| 1 | 0.083 | nd | - | 1.43 | nd | >30 | nd | 10.98 | nd | 17.2 | >360 | 132 |
| 2 | 0.076 | nd | - | 10.0 | nd | 10.71 | nd | 1.18 | nd | 175 | 188 | 16 |
| 3 | 0.00031 | nd | - | 4.57 | nd | 14.42 | nd | 0.334 | nd | 14,700 | 46,500 | 1077 |
| 4 | 0.19 | 0.012 | 15.8 | ∼30 | 2.6 | 13.27 | 12.9 | 22.48 | 0.92 | ∼217 | 1075 | 77 |
| 5 | 1.73 | 0.017 | 102 | 40.9 | 7.82 | 28.3 | 11.2 | >30 | ∼30 | 460 | 660 | ∼1750 |
| 6 | 1.9 | 0.0003 | 6333 | >30 | >30 | >30 | 18.84 | ∼30 | 1.28 | >100,000 | 62,800 | 4300 |
aWith 660 nm light, 58.7 J/cm2.
bDetermined by conversion of 7-ethoxyresorufin (REE).
cDetermined by conversion of dibenzylfluorescein (DBF).
dDetermined by conversion of 7-benzoyloxy-4-trifluoromethylcoumarin. The selectivity indices were calculated as the ratio of the IC50 values for different CYPs to CYP1B1 (for complexes 4–6 the IC50 (light) values were used). (n = 3).