Table 1. The inhibition assay against CA IX, CA I and CA II in vitro.
Compounds | IC50 (nM) |
Selectivity ratios (I/IX) | Selectivity ratios (II/IX) | ||
CA IX | CA I | CA II | |||
AZA | 7.72 | 509.60 | 37.59 | 66.01 | 4.87 |
EZA | 0.25 | 67.64 | 4.83 | 270.56 | 19.32 |
1a | 2.86 | 197.64 | 60.93 | 69.10 | 21.30 |
1b | 25.75 | 866.74 | 166.58 | 33.66 | 6.47 |
2a | 4.14 | 423.42 | 12.94 | 102.28 | 3.13 |
2b | 42.23 | 1541.18 | 239.58 | 36.50 | 5.67 |
3a | 3.42 | 660.65 | 22.86 | 193.17 | 6.68 |
3b | 18.98 | 772.88 | 276.83 | 40.72 | 14.58 |
4a | 0.47 | 693.64 | 25.58 | 1475.83 | 54.42 |
4b | 25.50 | 664.71 | 908.13 | 26.07 | 35.61 |
5a | 0.30 | 266.56 | 2.09 | 888.53 | 6.97 |
5b | 54.35 | 44.38 | 20.75 | 0.82 | 0.38 |
6a | 0.48 | 503.74 | 749.28 | 1049.46 | 1561 |
6b | >104 | 60.46 | 142.48 | — | — |
7a | 0.12 | 631.92 | 11.82 | 5266 | 98.50 |
7b | 4.42 | 1341.59 | 949.64 | 303.53 | 214.85 |