A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Kemp, MM; Wang, Q; Fuller, JH; West, N; Martinez, NM; Morse, EM; Weïwer, M; Schreiber, SL; Bradner, JE; Koehler, AN

Published Date

  • July 2011

Published In

Volume / Issue

  • 21 / 14

Start / End Page

  • 4164 - 4169

PubMed ID

  • 21696956

Pubmed Central ID

  • PMC3248787

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2011.05.098


  • eng