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A cyclodextrin-capped histone deacetylase inhibitor
journal contributionposted on 2023-06-08, 18:34 authored by Jahangir Amin, Antonio Puglisi, James Clarke, John Milton, Minghua Wang, Ronald M Paranal, James E Bradner, John SpencerJohn Spencer
We have synthesized a ß-cyclodextrin (ßCD)-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.
JournalBioorganic and Medicinal Chemistry Letters
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