Aromatic Sulfide Inhibitors of Histone Deacetylase Based on Arylsulfinyl-2,4-hexadienoic Acid Hydroxyamides

摘要

The synthesis of a novel series of potent inhibitors of histone deacetylases is described,based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides and their derivatives.In vitro IC_(50) values down to 40 nM were obtained,and several compounds showed inhibition of CEM (human leukemic) cell viability with IC_(50) of approx 1.5 mu M,comparable to or better than that of suberoylanilide hydroxamic acid,an inhibitor of histone deacetylase currently in clinical trials.