The Effect of Various Zinc Binding Groups on Inhibition of Histone Deacetylases 1-11

We discovered silanediol to be a novel functionality with potential as a suitable design element in the preparation of new Histone deacetylases inhibitors

Andreas S. Madsen; Helle M. E. Kristensen; Gyrithe Lanz; Christian A. Olsen

2013

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  • Zinc about it: We synthesized a series of compounds containing diverse zinc binding motifs and profiled their inhibitory activity against the 11 human histone deacetylases
  • We discovered silanediol to be a novel functionality with potential as a suitable design element in the preparation of new Histone deacetylases inhibitors
  • Given that human cells contain thousands of different acetylated lysine residues, HDACS may regulate a wide variety of processes including some implicated in conditions such as cancer and neurodegenerative disorders
  • By evaluating the compound collection against all 11 recombinant human HDACs, we found that the trifluoromethyl ketone functionality provides potent inhibition of all four subclasses of the Zn2+-dependent HDACs
  • Potent inhibition was observed with two different scaffolds, demonstrating the efficiency of the trifluoromethyl ketone moiety as a zinc binding motif
  • Any queries should be directed to the corresponding author for the article

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