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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 |
| Volume | 21 |
| Issue | 9 |
| Pages | 2601-5 |
| Date Published (YYYY/MM/DD) | 2011/05/01 |
| ISSN Number | 0960-894X |
| DOI | 10.1016/j.bmcl.2011.01.134 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/21334896?dopt=Abstract |
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