Table 5.
Effect of Building Block Modification on HDAC Inhibition
![]() | |||||||||
---|---|---|---|---|---|---|---|---|---|
entry | R | HDAC1 | IC50 (μM) HDAC2 |
HDAC3 | entry | R | HDAC1 | IC50 (μM) HDAC2 |
HDAC3 |
1 |
![]() |
2.7 ± 0.3 | 6.6 ± 0.4 | 2.7 ± 0.2 | 7 |
![]() |
>100 | >100 | >100 |
2 |
![]() |
1.5 ± 0.7 | 2.8 ± 0.9 | 4.4 ± 2.0 | 8 |
![]() |
59 ± 7 | 59 ± 14 | 39 ± 8 |
3 |
![]() |
30 ± 7 | 65 ± 40 | 22 ± 10 | 9 |
![]() |
>100 | >100 | >100 |
4 |
![]() |
33 ± 8 | 37 ± 6 | 23 ± 15 | 10 |
![]() |
>100 | >100 | >100 |
5 |
![]() |
5.0 ± 1.1 | 7.5 ± 0.8 | 3.9 ± 0.5 | 11 |
![]() |
>100 | >100 | >100 |
6 |
![]() |
>100 | >100 | >100 | 12 |
![]() |
>100 | >100 | >100 |