Table 1.
Compound | R1 | R2 | R3 | R4 | hHDAC1 (IC50 nM) | hHDAC6 (IC50 nM) | HDAC1/6 |
---|---|---|---|---|---|---|---|
(±)-6a | H | 4290 | 73.2 ± 11.6 | 59 | |||
(±)-6b | H | 3650 | 164.8 ± 30.7 | 22 | |||
(±)-6c | H | 8100 | 110.6 ± 15.5 | 73 | |||
(±)-6d | H | 4850 | 28.5 ± 3.8 | 170 | |||
(±)-6e | H | 6160 | 141.9 ± 38.6 | 43 | |||
(±)-6f | H | 7600 | 111.7 ± 19.4 | 68 | |||
(±)-6g | Me | H | 18680 | 166.2 ± 31.3 | 112 | ||
(±)-6h | Me | H | 5330 | 41.9 ± 6.0 | 127 | ||
(R)-(+)-6h | Me | H | 16190 | 90.6 ± 15.5 | 178 | ||
(S)-(−)-6h | Me | H | 3380 | 71.3 ± 8.4 | 47 | ||
(±)-6i | Me | OMe | 5320 | 67.2 ± 15.3 | 79 | ||
(±)-6j | Me | H | 6320 | 810.8 ± 59.6 | 8 | ||
(±)-6k | Me | H | 1630 | 616.3 ± 40.7 | 3 | ||
(±)-61 | Me | H | 10790 | 61.1 ± 12.9 | 177 | ||
(±)-6m | H | 8100 | 151.6 ± 26.4 | 53 | |||
Tubacin, 37 | - | - | - | - | 1400 | 4 | 350 |
SAHA, 47 | - | - | - | - | 33 | 33 | 1 |
Each value is the mean of at least three determinations; results are expressed with ±SD. When not specified, SD is <10% of the IC50.