Table 2.
Cytotoxicities of 10a-p against selected leukemia cell lines. Vorinostat, HPOB, and ricolinostat were used as controls.
Compound | R1 | R2 | HAL01 IC50 [μM] | HL60 IC50 [μM] | Jurkat IC50 [μM] |
---|---|---|---|---|---|
10a | c-Hexyl | 3,5-Me | 3.10 ± 0.91 | 2.47 ± 2.05 | 3.91 ± 0.67 |
10b | c -Hexyl | 4-NMe2 | 1.05±0.28 | 0.494±0.126 | 0.946±0.087 |
10c | c -Hexyl | 2-F | 11.8±5.14 | 6.79±3.31 | 8.97±1.73 |
10d | c -Hexyl | 2-Me | 9.93±1.55 | 7.72±3.45 | 9.47±3.55 |
10e | c -Hexyl | 2-OMe | >25 | 12.3±9.70 | 18.6±9.01 |
10f | c-Hexyl | 2-CF3 | 9.12±4.44 | 2.00±0.80 | >25 |
10g | Bn | 3,5-Me | 2.75±1.92 | 9.15±0.28 | 6.23±1.62 |
10h | Bn | 4-NMe2 | 0.375±0.162 | 0.218±0.122 | 0.285±0.064 |
10i | t-Bu | 3,5-Me | 4.93±2.60 | 4.84±2.78 | 5.47±0.86 |
10j | t-Bu | 4-NMe2 | 2.47±0.74 | 1.46±0.77 | 1.74±0.26 |
10k | t-Bu | 2-F | 22.2±3.8 | 15.7±6.87 | 19.0±4.58 |
10l | t-Bu | 2-Me | 23.9±1.54 | 13.6±8.19 | 23.9±1.49 |
10m | t-Bu | 2-OMe | >25 | 18.4±9.34 | 24.5±0.75 |
10n | t-Bu | 2-CF3 | >25 | 18.6±9.05 | >25 |
10o | t-Bu | 2-Cl | 22.9±2.64 | 12.8±8.66 | 21.6±3.37 |
10p | t-Bu | 2-iPr | >25 | 12.2±9.36 | >25 |
Vorinostat | - | - | 0.299±0.045 | 0.22±0.05 | 0.470±0.023 |
Ricolinostat | - | 2.04±0.39 | 1.54±0.16 | 2.42±0.18 | |
HPOB | - | - | 13.9±3.89 | 11.3±7.2 | 16.1±2.52 |