|Publication Type||Journal Article|
|Year of Publication||2011|
|Authors||Tang, W, Luo, T, Greenberg, EF, Bradner, JE, Schreiber, SL|
|Journal||Bioorganic & medicinal chemistry letters|
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.