Table 3 Inhibition data of human CA isoforms hCA I, II, IX and XII with 3-alkenyl-oxindole derivatives 4a-d, 5, 7, 91a–c, 111a–c, 131a–c, 151a–c and the standard inhibitor Acetazolamide (AAZ) by stopped flow CO2 hydrase assay
Ki (nM)* | Selectivity ratio | |||||||
|---|---|---|---|---|---|---|---|---|
Cmp | hCA I | hCAII | hCA IX | hCA XII | I/IX | I/XII | II/IX | II/XII |
4a |  > 10,000 | 8953 |  > 10,000 |  > 10,000 |  |  |  |  |
4b |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
4c | 6323 | 8669 |  > 10,000 |  > 10,000 |  |  |  |  |
4d | 8.4 | 3.9 | 84.2 | 8.7 | 0.100 | 0.966 | 0.046 | 0.448 |
5 | 6345 | 913.5 | 208.2 | 42.4 | 30.48 | 149.65 | 4.39 | 21.54 |
7 | 6236 | 5582 | 940.7 | 133.0 | 6.63 | 46.89 | 5.93 | 41.97 |
9a | 332.3 | 313.0 | 68.8 | 59.4 | 4.83 | 5.59 | 4.55 | 5.27 |
9b |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
9c |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
11a | 320.8 | 746.4 | 217.4 | 78.6 | 1.48 | 4.08 | 3.43 | 9.50 |
11b | 9108 | 2658 | 7856 | 8574 | 1.16 | 1.06 | 0.34 | 0.31 |
11c |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
13a | 483.0 | 306.6 | 91.3 | 182.7 | 5.29 | 2.64 | 3.36 | 1.68 |
13b |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
13c |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
15a | 844.5 | 762.5 | 863.3 | 175.0 | 0.98 | 4.83 | 0.88 | 4.36 |
15b |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
15c |  > 10,000 |  > 10,000 |  > 10,000 |  > 10,000 |  |  |  |  |
AAZ | 250.0 | 12.1 | 25.8 | 5.7 | 9.69 | 43.86 | 0.47 | 2.12 |