RESUMEN
A mini library of HDAC inhibitors with peptoid-based cap groups was synthesized using an efficient multicomponent approach. Four compounds were identified as potent HDAC6 inhibitors with a selectivity over other HDAC isoforms. The most potent HDAC6 inhibitor revealed remarkable chemosensitizing properties and completely reverted the cisplatin resistance in Cal27 CisR cells.
Asunto(s)
Inhibidores de Histona Desacetilasas/síntesis química , Peptoides/química , Diseño de Fármacos , Inhibidores de Histona Desacetilasas/química , Inhibidores de Histona Desacetilasas/farmacología , Simulación del Acoplamiento MolecularRESUMEN
By the reaction of diisopropylamine with concentrated hydrofluoric acid, the title compound, C(6)H(16)N(+).HF(2)(-), was synthesized. The cations and anions are connected via hydrogen bonds to form chains along [100]. The interlocked polymeric zigzag chains are hexagonally surrounded by six neighbouring chains. The F(-) anion is strongly hydrogen bonded to HF [F-H 0.98 (4), H...F 1.34 (4), F...F 2.3125 (16) A and F-H...F 174 (3) degrees]; a better description is that of a non-centred hydrogen difluoride anion.