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A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.

Publication ,  Journal Article
Kemp, MM; Wang, Q; Fuller, JH; West, N; Martinez, NM; Morse, EM; Weïwer, M; Schreiber, SL; Bradner, JE; Koehler, AN
Published in: Bioorganic & medicinal chemistry letters
July 2011

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.

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Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

July 2011

Volume

21

Issue

14

Start / End Page

4164 / 4169

Related Subject Headings

  • Structure-Activity Relationship
  • Pyrimidines
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Histone Deacetylases
  • Histone Deacetylase Inhibitors
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0305 Organic Chemistry
  • 0304 Medicinal and Biomolecular Chemistry
 

Citation

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Kemp, M. M., Wang, Q., Fuller, J. H., West, N., Martinez, N. M., Morse, E. M., … Koehler, A. N. (2011). A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. Bioorganic & Medicinal Chemistry Letters, 21(14), 4164–4169. https://doi.org/10.1016/j.bmcl.2011.05.098
Kemp, Melissa M., Qiu Wang, Jason H. Fuller, Nathan West, Nicole M. Martinez, Elizabeth M. Morse, Michel Weïwer, Stuart L. Schreiber, James E. Bradner, and Angela N. Koehler. “A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.Bioorganic & Medicinal Chemistry Letters 21, no. 14 (July 2011): 4164–69. https://doi.org/10.1016/j.bmcl.2011.05.098.
Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, et al. A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. Bioorganic & medicinal chemistry letters. 2011 Jul;21(14):4164–9.
Kemp, Melissa M., et al. “A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.Bioorganic & Medicinal Chemistry Letters, vol. 21, no. 14, July 2011, pp. 4164–69. Epmc, doi:10.1016/j.bmcl.2011.05.098.
Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, Weïwer M, Schreiber SL, Bradner JE, Koehler AN. A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. Bioorganic & medicinal chemistry letters. 2011 Jul;21(14):4164–4169.
Journal cover image

Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

July 2011

Volume

21

Issue

14

Start / End Page

4164 / 4169

Related Subject Headings

  • Structure-Activity Relationship
  • Pyrimidines
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Histone Deacetylases
  • Histone Deacetylase Inhibitors
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0305 Organic Chemistry
  • 0304 Medicinal and Biomolecular Chemistry