Table 2.
Compound |
Ki (nM)a
|
Selectivity Ratiob
|
|||||
---|---|---|---|---|---|---|---|
hCA II | hCA IX | hCA XII | II/IX | II/XII | IX/XII | XII/IX | |
U-CH3 | 1765 | 7 | 6 | 250 | 300 | 1 | 1 |
U-F | 960 | 45 | 4 | 20 | 240 | 10 | <1 |
U-NO2 | 15 | 1 | 6 | 15 | 2 | <1 | 5 |
Ki values obtained from Pacchiano et al., [11]: U-CH3 (3,5-Me2C6H3), U-F (4-FC6H4), U-NO2 (3-O2NC6H4).
Selectivity as determined by the ratio of Kis for hCA isozyme relative to hCA IX and hCA XII.