Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 14, Pages 3928-3931Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.085
Keywords
HDAC; Cyclic tetrapeptide; Solid-phase peptide synthesis
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Funding
- National Institutes of Health [R21-NS055781]
- Repligen Corporation, Waltham, MA
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We designed and synthesized a series of novel hybrid histone deacetylase inhibitors based on conjugation of benzamide-type inhibitors with either linear or cyclic peptides. Linear tetrapeptides (compounds 13 and 14), cyclic tetrapeptides (compounds 1 and 11), and heptanediamide-peptide conjugates (compounds 10, 12, 15 and 16) were synthesized through on-resin solid-phase peptide synthesis (SPPS). All compounds were found to be moderate HDAC1 and HDAC3 inhibitors, with IC50 values ranging from 1.3 mu M to 532 mu M. Interestingly, compound 15 showed 19-fold selectivity for HDAC3 versus HDAC1. (C) 2009 Elsevier Ltd. All rights reserved.
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