Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides |
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| Authors: | Marson Charles M Savy Pascal Rioja Alphonso S Mahadevan Thevaki Mikol Catherine Veerupillai Arthi Nsubuga Eva Chahwan Angela Joel Simon P |
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| Affiliation: | Department of Chemistry, University College London, Christopher Ingold Laboratories, London WC1H OAJ, UK. c.m.marson@ucl.ac.uk |
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| 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 IC(50) values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC(50) of approximately 1.5 microM, comparable to or better than that of suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase currently in clinical trials. |
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