Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2011 May 1;21(9):2601-5. doi: 10.1016/j.bmcl.2011.01.134. Epub 2011 Feb 2.

Discovery of histone deacetylase 8 selective inhibitors.

Author information

1
Howard Hughes Medical Institute, Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA. wtang@pharmacy.wisc.edu

Abstract

We have developed an efficient method for synthesizing candidate histone deacetylase (HDAC) inhibitors in 96-well plates, which are used directly in high-throughput screening. We selected building blocks having hydrazide, aldehyde and hydroxamic acid functionalities. The hydrazides were coupled with different aldehydes in DMSO. The resulting products have the previously identified 'cap/linker/biasing element' structure known to favor inhibition of HDACs. These compounds were assayed without further purification. HDAC8-selective inhibitors were discovered from this novel collection of compounds.

PMID:
21334896
PMCID:
PMC3403710
DOI:
10.1016/j.bmcl.2011.01.134
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

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