Table 5
AR binding affinity of bicalutamide derivatives bearing coumarin ring
| Compound | 6 or 7 Substitution | R1 | X | R2 | Ki |
|---|---|---|---|---|---|
| nM | |||||
| 45 | 6 | H | S | F | >1500 |
| 46 | 7 | CH3 | S | F | 91 ± 8 |
| 47 | 7 | CH3 | SO2 | F | 80 ± 16 |
| 48 | 7 | CF3 | S | H | 133 ± 2 |
| 49 | 7 | CF3 | S | F | 336 ± 30 |
| 50 | 7 | CF3 | S | NCS | 136 ± 5 |
| 51 | 7 | CF3 | S | NH2 | 289 ± 30 |
| 52 | 7 | CF3 | S | NHCOCH3 | >1500 |
K i values were determined from the competitive binding assay, as described under Materials and Methods. Values represent the mean ± S.D. of at least three experiments.
