Scientific Publications

Discovery of histone deacetylase 8 selective inhibitors.

Publication TypeJournal Article
AuthorsTang, W., Luo T., Greenberg EF, Bradner JE, and Schreiber SL
AbstractWe 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.
Year of Publication2011
JournalBioorganic & medicinal chemistry letters
Volume21
Issue9
Pages2601-5
Date Published (YYYY/MM/DD)2011/05/01
ISSN Number0960-894X
DOI10.1016/j.bmcl.2011.01.134
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/21334896?dopt=Abstract