Format

Send to

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4164-9. doi: 10.1016/j.bmcl.2011.05.098. Epub 2011 Jun 2.

A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.

Author information

1
Broad Institute of Harvard and MIT, Cambridge, MA 02142, United States.

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.

PMID:
21696956
PMCID:
PMC3248787
DOI:
10.1016/j.bmcl.2011.05.098
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science Icon for PubMed Central
    Loading ...
    Support Center