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Bioorganic & medicinal chemistry letters DOI:10.1016/j.bmcl.2011.01.134

Discovery of histone deacetylase 8 selective inhibitors.

Publication TypeJournal Article
Year of Publication2011
AuthorsTang, W, Luo, T, Greenberg, EF, Bradner, JE, Schreiber, SL
JournalBioorganic & medicinal chemistry letters
Volume21
Issue9
Pages2601-5
Date Published2011/05/01
ISSN0960-894X
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.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S0960-894X(11)00168-5
DOI10.1016/j.bmcl.2011.01.134
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/21334896?dopt=Abstract