Cytotoxicity of belinostat derivatives against MOPC-315 cell line.
Compd | A position | IC50 (μM) | Fold change |
---|---|---|---|
7a | 4-Fluorobenzyl | 0.457 ± 0.033 | 0.695 |
7b | 4-Methylbenzyl | 0.167 ± 0.014 | 1.907 |
7c | Benzyl | 0.291 ± 0.044 | 1.093 |
7d | Cyclohexyl | 0.444 ± 0.181 | 0.714 |
7e | 5-Fluoro-2-methylphenyl | 0.380 ± 0.073 | 0.835 |
7fa | 4-Methoxyphenyl | 0.090 ± 0.016 | 3.522 |
7g | 4-Methylphenyl | 0.159 ± 0.046 | 1.993 |
7h | 4-Chloro-2-fluorophenyl | 1.029 ± 0.469 | 0.309 |
7i | 4-Fluorophenyl | 0.312 ± 0.114 | 1.019 |
7j | 2,4-Difluorophenyl | 0.784 ± 0.198 | 0.405 |
7k | 3-Fluorophenyl | 0.365 ± 0.019 | 0.869 |
7l | (Z)-4-(1-(Hydroxyimino)ethyl)phenyl | 2.141 ± 1.246 | 0.148 |
Belinostat b | Phenyl | 0.318 ± 0.049 | 1.000 |
Compound 7f was chosen for further studies.
Belinostat was used as a positive control.