2. Academic Validation
  3. New aryldithiolethione derivatives as potent histone deacetylase inhibitors

New aryldithiolethione derivatives as potent histone deacetylase inhibitors

  • Bioorg Med Chem. 2010 Jun 15;18(12):4187-94. doi: 10.1016/j.bmc.2010.05.011.
Valerio Tazzari 1,  Graziella Cappelletti,  Manolo Casagrande,  Elena Perrino,  Luigi Renzi,  Piero Del Soldato,  Anna Sparatore
Affiliations

Affiliation

  • 1 Sulfidris s.r.l., Viale Gran Sasso 17, 20131 Milan, Italy.
PMID: 20576572 DOI: 10.1016/j.bmc.2010.05.011
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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