Discovery of histone deacetylase 8 selective inhibitors.
Bioorg Med Chem Lett
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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. |
| Year of Publication | 2011
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| Journal | Bioorg Med Chem Lett
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| Volume | 21
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| Issue | 9
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| Pages | 2601-5
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| Date Published | 2011 May 01
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| ISSN | 1464-3405
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| DOI | 10.1016/j.bmcl.2011.01.134
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| PubMed ID | 21334896
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| PubMed Central ID | PMC3403710
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| Grant list | Howard Hughes Medical Institute / United States
K08 CA128972 / CA / NCI NIH HHS / United States
R01 GM038627 / GM / NIGMS NIH HHS / United States
NIGMS 38627 / PHS HHS / United States
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