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J Med Chem. 2007 May 3;50(9):2003-6. Epub 2007 Apr 10.

Design and synthesis of a potent histone deacetylase inhibitor.

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1
Virginia Tech, Department of Chemistry MC 0212, Blacksburg, Virginia 24061-0212, USA.

Abstract

Histone deacetylase (HDAC) inhibitors have potential for cancer therapy. An HDAC inhibitor based on a cyclic peptide mimic of known structure, linked by an aliphatic chain to a hydroxamic acid, was designed and synthesized. The chimeric compound showed potent competitive inhibition of nuclear HDACs, with an IC50 value of 46 nM and a Ki value of 13.7 nM. The designed inhibitor showed 4-fold selectivity for HDAC1 (57 nM) over HDAC8 (231 nM).

PMID:
17419603
DOI:
10.1021/jm061082q
[Indexed for MEDLINE]
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