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Updated: Jun 12, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
New aryldithiolethione derivatives as potent histone deacetylase inhibitors
Valerio Tazzari1, Graziella Cappelletti, Manolo Casagrande
1Sulfidris s.r.l., Viale Gran Sasso 17, 20131 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 IC(50) 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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