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ID: ALA1770095

Journal: Bioorg Med Chem Lett

Title: Discovery of histone deacetylase 8 selective inhibitors.

Authors: Tang W, Luo T, Greenberg EF, Bradner JE, Schreiber SL.

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.

CiteXplore: 21334896

DOI: 10.1016/j.bmcl.2011.01.134