A cyclodextrin-capped histone deacetylase inhibitor

Amin, Jahangir, Puglisi, Antonio, Clarke, James, Milton, John, Wang, Minghua, Paranal, Ronald M, Bradner, James E and Spencer, John (2013) A cyclodextrin-capped histone deacetylase inhibitor. Bioorganic and Medicinal Chemistry Letters, 23 (11). pp. 3346-3348. ISSN 0960-894X

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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.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science
Depositing User: Deeptima Massey
Date Deposited: 30 Sep 2014 11:15
Last Modified: 11 May 2015 11:06
URI: http://sro.sussex.ac.uk/id/eprint/50419
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