Table 3

AR binding affinity of racemic bicalutamide derivatives

CompoundR1XR2Ki
nM
27CNSNO2 19  ± 5
28NO2 SNO2 20  ± 2
29NO2 SNHCOCH3 2.5  ± 0.13-150
30NO2 SNHCOCH2Cl5.0  ± 0.63-150
31NO2 SO2 NHCOCH2Cl5.0  ± 0.73-150

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

    • ↵3-150  Significantly lower K i than that of (R)-bicalutamide (R-1) with P < 0.05.