Table 1.
In vitro inhibition of selected carbonic anhydrase isoenzymes [75].
Compound | Linker, Stereochemistry or Substitution |
Ki (CA-II) [nM] |
Ki (CA-IX) [nM] |
Selectivity Index [a] |
---|---|---|---|---|
95−1 | Mono, C2 | 133.10 ± 15.35 | 0.92 ± 0.28 | 144.2 |
91a− | Mono, C2, Cl2 | 29.85 ± 4.46 | 0.89 ± 0.15 | 33.5 |
91b− | Mono, C3, Cl2 | 8.10 ± 0.86 | 0.10 ± 0.02 | 82.7 |
93a− | C1, rac- | 41.09 ± 6.09 | 0.86 ± 0.12 | 47.6 |
93b− | C2, rac- | 164.90 ± 19.86 | 0.86 ± 0.15 | 191.5 |
94a− | C2, meso- | 74.17 ± 12.67 | 0.37 ± 0.05 | 199.9 |
93c− | C3, rac- | 11.36 ± 1.25 | 0.02 ± 0.003 | 668.2 |
94b− | C3, meso- | 26.76 ± 2.45 | 0.60 ± 0.12 | 44.5 |
93d− | C4, rac- | 10.07 ± 0.61 | 0.29 ± 0.01 | 35.2 |
94c− | C4, meso- | 31.57 ± 3.69 | 0.06 ± 0.01 | 574.0 |
[a] Selectivity index is the ratio between Ki (CA-II) and Ki (CA-IX).