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Updated: May 12, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
A cyclodextrin-capped histone deacetylase inhibitor
Jahangir Amin1, Antonino Puglisi, James Clarke
1Dept. of Chemistry, School of Life Sciences, University of Sussex, Falmer, Brighton BN1 9QJ, East Sussex, UK. j.amin@sussex.ac.uk
Abstract:
We have synthesized a β-cyclodextrin (βCD)-capped histone deacetylase (HDAC) inhibitor 3 containing an alkyl linker and a zinc-binding hydroxamic acid motif. Biological evaluation (HDAC inhibition studies) of 3 enabled us to establish the effect of replacing an aryl cap (in SAHA (vorinostat,)) 1 by a large saccharidic scaffold "cap". HDAC inhibition was observed for 3, to a lesser extent than SAHA, and rationalized by molecular docking into the active site of HDAC8. However, compound 3 displayed no cellular activity.
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