Table 1.
Inhibition data of human CA isoforms hCA I, II, IV and IX with compounds reported here and the standard sulfonamide inhibitor acetazolamide (AAZ) by a stopped flow CO2 hydrase assay.
| KI (µM)* |
||||
|---|---|---|---|---|
| Compound | hCAI | hCA II | hCA IV | hCA IX |
| Chenodeoxycholic acid (1) | >100 | 53.9 | >100 | 63.0 |
| Cholic acid (2) | >100 | 48.9 | >100 | 47.1 |
| Lithocholic acid (3) | >100 | 64.5 | >100 | 70.2 |
| Deoxycholic acid (4) | >100 | 51.0 | >100 | 55.0 |
| Ursodeoxycholic acid (5) | 95.9 | 71.4 | >100 | 73.1 |
| Glycoursodeoxycholic acid (6) | >100 | 78.4 | >100 | 89.9 |
| Tauroursodeoxycholic acid (7) | >100 | 82.9 | >100 | 42.9 |
| Hyodeoxycholic acid (8) | >100 | 58.4 | >100 | 67.7 |
| Hyocholic acid (9) | 83.3 | 38.9 | >100 | 71.9 |
| Dehydrocholic acid (10) | >100 | 57.8 | >100 | 53.9 |
| Cholesterol (11) | >100 | >100 | >100 | >100 |
| Coprostan-3-ol (12) | >100 | >100 | >100 | >100 |
| Testosterone (13) | >100 | >100 | >100 | >100 |
| Androsterone (14) | >100 | >100 | >100 | >100 |
| Trans-dehydroandrosterone (15) | >100 | >100 | >100 | >100 |
| Androstanolone (16) | >100 | >100 | >100 | >100 |
| Progesterone (17) | >100 | >100 | >100 | >100 |
| 11α-Hydroxyprogesterone (18) | >100 | >100 | >100 | >100 |
| α-Estradiol (19) | 87.8 | 40.4 | >100 | 49.6 |
| Estron (20) | >100 | 50.8 | >100 | 71.4 |
| Hydrocortisone (21) | >100 | >100 | >100 | >100 |
| Diosgenin (22) | >100 | >100 | >100 | >100 |
| AAZ | 0.25 | 0.012 | 0.074 | 0.025 |
*
Mean from 3 different assays, by a stopped flow technique (errors were in the range of ±5–10% of the reported values).