Table 1.
In VitroAnti-HDAC Activity (IC50) and Isoform Selectivity of Non-Peptide Macrocyclic HDACi
| Compound | HDAC 1/2 (nM) | HDAC 8 (μM) | Isoform Selectivity |
|---|---|---|---|
| 10 | 107.1 | 6.68 | 62 |
| 11 | 109.8 | 2.32 | 21 |
| 12a | 91.6 | 4.73 | 51.63 |
| 12b | 13.9 | 0.99 | 71.77 |
| 12c | 58.9 | 7.13 | 121 |
| 12d | 145.5 | 11.05 | 38 |
| 12e | 226.7 | ND | c |
| 13a | 88.8 | 3.74 | 42.11 |
| 13b | 10.6 | 1.02 | 96.59 |
| 13c | 72.4 | 6.78 | 94 |
| 14a | 37.0 | 3.99 | 107.90 |
| 14b | 4.1 | 1.89 | 462.10 |
| 14c | 55.6 | 5.88 | 106 |
| 14d | 169.8 | 10.55 | 56 |
| 14e | 223.4 | ND | c |
| 15a | 44.3 | 4.75 | 107.32 |
| 15b | 1.9 | 1.39 | 743.32 |
| 15c | 123.0 | 4.42 | 36 |
| SAHA | 65 | 1.86 | 28.61 |