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Discovery of histone deacetylase 8 selective inhibitors.
|Publication Type||Journal Article|
|Authors||Tang, W., Luo T., Greenberg EF, Bradner JE, and 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.|
|Year of Publication||2011|
|Journal||Bioorganic & medicinal chemistry letters|
|Date Published (YYYY/MM/DD)||2011/05/01|