Table 1.
HDAC class I cellular activity and in vitro antiproliferative activity for synthesized HDAC inhibitors 3, 11a, 19, 22, 30a, 30b and 37.a
Cpd No. | Structure | IC50 of HDAC cellular class I (μM)b | IC50 of HL60 cell (μM) |
---|---|---|---|
3 |
![]() |
0.85 | 2.14 |
11a |
![]() |
0.67 | 1.84 |
19 |
![]() |
1.23 | 7.94 |
30a |
![]() |
0.82 | 1.93 |
30b |
![]() |
>10 | >20 |
22 |
![]() |
1.75 | 5.97 |
37 |
![]() |
2.95 | 8.04 |
MS275 |
![]() |
0.62 | 1.52 |
Assays were performed in HL60 cells; Values are average of at least two determinations, the SD values are < 20% of the mean.
Boc-Lys (acetyl)-AMC substrate.