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. Author manuscript; available in PMC: 2023 Nov 24.
Published in final edited form as: J Med Chem. 2022 Nov 9;65(22):15457–15472. doi: 10.1021/acs.jmedchem.2c01418

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