Table 1. Inhibitory Activity against Human HDACs.
IC50 (μM)d |
|||||
---|---|---|---|---|---|
compd | R1 | R2 | HDAC1 | HDAC3 | HDAC6 |
1aa | n-C7H15CO | 0.0137 | 0.2450 | 11.50 | |
1bb | H | 0.0012 | 0.0034 | 0.049 | |
2aa | n-C7H15CO | 2.0 | 16.8 | 14.7 | |
2bb | H | 0.077 | 0.085 | >30 | |
3a | H | n-C7H15CO | 1.90 ± 0.25 | 2.83 ± 0.34 | NAc |
3b | H | H | 0.09 ± 0.02 | 0.06 ± 0.01 | 3.71 ± 0.27 |
3c | Me | n-C7H15CO | 2.60 ± 0.45 | 3.56 ± 0.44 | NA |
3d | Me | H | 0.12 ± 0.02 | 0.11 ± 0.02 | 4.32 ± 0.33 |
4a | H | n-C7H15CO | NAc | NAc | NAc |
4b | H | H | 16.82 ± 1.0 | NAc | NAc |
4c | Me | n-C7H15CO | NAc | NAc | NAc |
4d | Me | H | 13.86 ± 2.2 | NAc | NAc |