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.
New aryldithiolethione derivatives as potent histone deacetylase inhibitors / V. Tazzari, G. Cappelletti, M. Casagrande, E. Perrino, L. Renzi, P. Del Soldato, A. Sparatore. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 18:12(2010 Jun 15), pp. 4187-4194.
New aryldithiolethione derivatives as potent histone deacetylase inhibitors
V. TazzariPrimo
;G. CappellettiSecondo
;M. Casagrande;A. Sparatore
2010
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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