Table 2

AR binding affinity of bicalutamide A- and B-ring derivatives

Ki
CompoundXRR-isomerS-isomer
nM
18SNH2 57  ± 2528  ± 26
19SNHCOCH3 2.9  ± 0.22-150 123  ± 27
20SO2 NHCOCH3 9.3  ± 0.8589  ± 127
21SNHCOCF3 2.6  ± 0.42-150 N.S.
22SO2 NHCOCF3 6.2  ± 1.12-150 N.S.
23SNHCOCH2Cl3.3  ± 0.42-150 97  ± 7
24SO2 NHCOCH2Cl6.9  ± 1.22-150 233  ± 74
25SNHSO2CH3 50  ± 1N.S.
26SO2 NHSO2CH3 15  ± 2N.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.                      


Embedded Image
    • 2-150  Significantly lower K i than that of (R)-bicalutamide (R-1) with P < 0.05.

    • N.S., not synthesized.