| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376803 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
One dithiolthione and two new methanethiosulfonate derivatives of valproic acid (VPA) were synthesized and tested in vitro as histone deacetylase (HDAC) inhibitors. The new molecules, as well as their sulfurated moieties, exhibited a much stronger inhibition of HDAC enzymatic and antiproliferative activities and histone hyperacetylation than VPA. ACS 2 is the most interesting compound among the new VPA derivatives and its sulfurated moiety, 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione, also known to be a metabolite of anethole trithione, seems to contribute significantly to its activity. This is the first time that HDAC inhibitory activity is described for dithiolethiones and thiosulfonates.
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Physical Sciences and Engineering
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Organic Chemistry
Authors
Elena Perrino, Graziella Cappelletti, Valerio Tazzari, Erminio Giavini, Piero Del Soldato, Anna Sparatore,