Discovery of histone deacetylase 8 selective inhibitors.

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Tang W, Luo T, Greenberg EF, Bradner JE, Schreiber SL

Discovery of histone deacetylase 8 selective inhibitors.

Bioorg Med Chem Lett. 2011 May 1;21(9):2601-5. doi: 10.1016/j.bmcl.2011.01.134. Epub 2011 Feb 2.

PubMed ID

21334896 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Vorinostat	Histone deacetylase 2	IC 50 (nM)	66	N/A	N/A	Details
Vorinostat	Histone deacetylase 3	IC 50 (nM)	34	N/A	N/A	Details