Literature DB >> 16420064

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

Charles M Marson1, Pascal Savy, Alphonso S Rioja, Thevaki Mahadevan, Catherine Mikol, Arthi Veerupillai, Eva Nsubuga, Angela Chahwan, Simon P Joel.   

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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Year:  2006        PMID: 16420064     DOI: 10.1021/jm051010j

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  1 in total

1.  Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.

Authors:  Katerina Capková; Yoshiyuki Yoneda; Tobin J Dickerson; Kim D Janda
Journal:  Bioorg Med Chem Lett       Date:  2007-10-09       Impact factor: 2.823

  1 in total

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