1316860-95-3Relevant academic research and scientific papers
Discovery of histone deacetylase 8 selective inhibitors
Tang, Weiping,Luo, Tuoping,Greenberg, Edward F.,Bradner, James E.,Schreiber, Stuart L.
, p. 2601 - 2605 (2011/06/22)
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.
