Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 14, Pages 4164-4169Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.098
Keywords
Histone deacetylase; Non-selective inhibitor; Hydroxy-pyrimidine; SAR studies
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Funding
- National Institute of General Medical Sciences (NIGMS) [38627]
- National Cancer Institute's Initiative for Chemical Genetics (ICG) [N01-CO-12400]
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Histone deacetylases (HDACs) are enzymes involved in many important biological functions. They have been linked to a variety of cancers, psychiatric disorders, and other diseases. Since small molecules can serve as probes to study the relevant biological roles of HDACs, novel scaffolds are necessary to develop more efficient, selective drug candidates. Screening libraries of molecules may yield structurally diverse probes that bind these enzymes and modulate their functions in cells. Here we report a small molecule with a novel hydroxy-pyrimidine scaffold that inhibits multiple HDAC enzymes and modulates acetylation levels in cells. Analogs were synthesized in an effort to evaluate structure-activity relationships. (C) 2011 Elsevier Ltd. All rights reserved.
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