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Bioorganic & medicinal chemistry letters DOI:10.1016/j.bmcl.2011.05.098

A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.

Publication TypeJournal Article
Year of Publication2011
AuthorsKemp, MM, Wang, Q, Fuller, JH, West, N, Martinez, NM, Morse, EM, Weïwer, M, Schreiber, SL, Bradner, JE, Koehler, AN
JournalBioorganic & medicinal chemistry letters
Volume21
Issue14
Pages4164-9
Date Published2011/07/15
ISSN0960-894X
Abstract

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.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S0960-894X(11)00739-6
DOI10.1016/j.bmcl.2011.05.098
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/21696956?dopt=Abstract