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New aryldithiolethione derivatives as potent histone deacetylase inhibitors |
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| Authors: | Valerio Tazzari Graziella Cappelletti Manolo Casagrande Elena Perrino Luigi Renzi Piero Del Soldato Anna Sparatore |
| Institution: | 1. Sulfidris s.r.l., Viale Gran Sasso 17, 20131 Milan, Italy;2. Department of Biology, University of Milan, Via Celoria 26, 20133 Milan, Italy;3. Department of Pharmaceutical Science ‘Pietro Pratesi’, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milan, Italy |
| Abstract: | A series of dithiolethione derivatives was synthesized and the in vitro HDAC inhibitory activity was tested. The most active compounds, 1 and 2, exhibited an IC50 in nM range with a strong hyperacetylation of histone H4 in A549 cells. The HDAC inhibitory activity comparable to that of SAHA and the inhibition of A549 cell proliferation suggest that these compounds are worthy of further studies as potential anticancer agents. |
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