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. Tazzari
Primo
;
G. Cappelletti
Secondo
;
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.
Anticancer agents; Dithiolethione derivatives; Histone deacetylase inhibitor
Settore CHIM/08 - Chimica Farmaceutica
15-giu-2010
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/143440
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