Table 3.
Selectivity index (SI) of series (A), (B) and AAZ toward tumor related hCA IX & XII over the off-target hCA I & II.
| Compound* | Selectivity index (SI) | |||
|---|---|---|---|---|
| I/IX | II/IX | I/XII | II/XII | |
| 5a | 6.7 | 6.8 | 0.3 | 0.2 |
| 6a | 0.6 | 0.8 | 0.1 | 0.2 |
| 6b | 0.4 | 0.8 | 0.1 | 0.2 |
| 6c | 0.1 | 0.1 | 0.02 | 0.04 |
| 7a | 23.2 | 1.3 | 1.5 | 0.1 |
| 8a | 0.1 | 2.5 | 0.01 | 0.5 |
| 8b | 0.2 | 1.4 | 0.1 | 0.6 |
| 8c | 0.3 | 0.5 | 0.4 | 0.6 |
| 10 | 0.03 | 0.02 | 0.01 | 0.006 |
| 12a | 2.3 | 0.3 | 0.4 | 0.05 |
| 12b | 2.5 | 2 | 0.3 | 0.2 |
| 12c | 0.7 | 1.4 | 0.1 | 0.2 |
| 12d | 3 | 2 | 3 | 2 |
| 12e | 4 | 1 | 0.5 | 0.1 |
| 12f. | 3 | 2.5 | 0.1 | 0.1 |
| 12g | 0.8 | 3.6 | 0.07 | 0.3 |
| 12h | 9.7 | 6.1 | 5.8 | 3.6 |
| 12i | 12.4 | 6.5 | 2.6 | 1.4 |
| 12j | 5.5 | 4.1 | 5.9 | 4.3 |
| AAZ | 9.7 | 0.5 | 43.9 | 2.1 |
*Compounds with Ki < 10,000 aren’t shown.