Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2, 4-hexadienoic acid hydroxyamides

…, P Savy, AS Rioja, T Mahadevan, C Mikol…

Index: Marson, Charles M.; Savy, Pascal; Rioja, Alphonse S.; Mahadevan, Thevaki; Mikol, Catherine; Veerupillai, Arthi; Nsubuga, Eva; Chahwan, Angela; Joel, Simon P. Journal of Medicinal Chemistry, 2006 , vol. 49, # 2 p. 800 - 805

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Citation Number: 16

Abstract

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 IC50 values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC50 of~ 1.5 μM, comparable to or better than that of suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase currently in clinical ...