Discovery of histone deacetylase 8 selective inhibitors |
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Authors: | Tang Weiping Luo Tuoping Greenberg Edward F Bradner James E Schreiber Stuart L |
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Affiliation: | Howard Hughes Medical Institute, Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA |
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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. |
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Keywords: | HDAC HDAC8 Macrocycle Inhibitor Hydroxamic acid |
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