doi: 10.1021/jm061082q.
Epub 2007 Apr 10.
Design and synthesis of a potent histone deacetylase inhibitor
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- PMID: 17419603
- DOI: 10.1021/jm061082q
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Design and synthesis of a potent histone deacetylase inhibitor
J Med Chem.
.
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).
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