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

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

  • J Med Chem. 2006 Jan 26;49(2):800-5. doi: 10.1021/jm051010j.
Charles M Marson 1,  Pascal Savy,  Alphonso S Rioja,  Thevaki Mahadevan,  Catherine Mikol,  Arthi Veerupillai,  Eva Nsubuga,  Angela Chahwan,  Simon P Joel
Affiliations

Affiliation

  • 1 Department of Chemistry, University College London, Christopher Ingold Laboratories, London WC1H OAJ, UK. c.m.marson@ucl.ac.uk
PMID: 16420064 DOI: 10.1021/jm051010j
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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