Ki | |||||
---|---|---|---|---|---|
Compound | R1 | X | R2 | R-isomer | S-isomer |
nM | |||||
1 (Bicalutamide) | OH | SO2 | p-F | 11 ± 21-a | 365 ± 101-a |
2 | OH | S | p-NH2 | 91 ± 161-a | >1500 |
3 | OH | SO | p-NH2 | >1500 | N.S. |
4 | OH | SO2 | p-NH2 | 32 ± 4 | N.S. |
5 | OH | S | p-NHCOCH3 | 4.9 ± 0.21-150 | 1370 ± 30 |
6 | OH | S | p-N(COCH3)2 | 104 ± 8 | N.S. |
7 | OH | SO2 | p-NHCOCH3 | 16 ± 1 | N.S. |
8 | OH | S | p-NHCOCH2CH3 | 27 ± 2 | N.S. |
9 | OH | S | p-N(COCH2CH3)2 | 658 ± 42 | N.S. |
10 | OH | S | p-NHCOCH2Br | 109 ± 6 | N.S. |
11 | OH | S | m-NHCOCH2Br | >1500 | N.S. |
12 | OH | S | p-NHCOCH2Cl | 1.7 ± 0.11-a 1-150 | 410 ± 49 |
13 | OH | SO2 | p-NHCOCH2Cl | 7.0 ± 0.91-150 | N.S. |
14 | OH | SO2 | m-NHCOCH2Cl | 43 ± 1 | N.S. |
15 | OH | S | m-NCS | 238 ± 14 | 956 ± 65 |
16 | OH | SO2 | p-Sn(CH3)3 | 117 ± 25 | N.S. |
17 | OCOCH3 | S | p-N(COCH2CH3)2 | >1500 | N.S. |
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.