Table 1. Ki Values (nM) against hCA I, hCA II, hCA VII, hCA IX, hCA XII, and hCA XIV Isoforms Shown by New Benzenesulfonamide Derivatives 5a–s and Reference Compounds 1 and 2, AAZ, and SLC-0111.
|
Ki (nM)a |
||||||
|---|---|---|---|---|---|---|
| hCA I | hCA II | hCA VII | hCA IX | hCA XII | hCA XIV | |
| 1 | 6.8 | 3.0 | 10.4 | 33.1 | 3.8 | 34.6 |
| 2 | 0.69 | 0.5 | 7.8 | 45.1 | 5.6 | 15.2 |
| 5a | 69.1 | 3.7 | 70.7 | 37.1 | 8.5 | 85.5 |
| 5b | 22.4 | 28.4 | 6.8 | 68.7 | 3.1 | 6.9 |
| 5c | 0.84 | 0.41 | 66.1 | 3.8 | 29.1 | 35.7 |
| 5d | 7.7 | 32.4 | 39.5 | 332.4 | 26.4 | 69.6 |
| 5e | 94.4 | 5.6 | 2.9 | 62.2 | 63.1 | 86.1 |
| 5f | 72.5 | 22.5 | 7.5 | 54.4 | 66.9 | 58.3 |
| 5g | 87.5 | 7.2 | 61.7 | 29.2 | 6.3 | 63.4 |
| 5h | 58.0 | 3.0 | 45.3 | 60.4 | 48.7 | 73.9 |
| 5i | 460 | 0.6 | 3.5 | 16.2 | 8.5 | 85.3 |
| 5j | 85.1 | 4.4 | 9.1 | 8.0 | 37.4 | 86.0 |
| 5k | 81.9 | 19.8 | 27.7 | 250.0 | 39.6 | 78.1 |
| 5l | 87.6 | 36.3 | 46.7 | 360.3 | 26.5 | 48.0 |
| 5m | 81.9 | 5.5 | 9.3 | 223.0 | 86.3 | 9.7 |
| 5n | 81.2 | 42.4 | 39.2 | 9.8 | 6.9 | 61.6 |
| 5o | 93.8 | 28.6 | 41.7 | 2.2 | 8.2 | 66.5 |
| 5p | 60.8 | 23.9 | 64.2 | 11.2 | 6.2 | 46.1 |
| 5q | 9.4 | 4.1 | 9.0 | 19.1 | 27.4 | 86.4 |
| 5r | 404.9 | 51.1 | 65.0 | 15.2 | 7.7 | 91.7 |
| 5s | 173.5 | 78.8 | 69.3 | 14.3 | 8.2 | 66.5 |
| AAZ | 250 | 12.5 | 2.5 | 25.8 | 5.7 | 41.0 |
| SLC-0111 | 5080 | 960.0 | 8550 | 45.0 | 4.5 | ND |
a
Errors are in the range of ±10% of the reported value, from three different assays. ND: not determined.