New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
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.
Tazzari
Valerio
V
Sulfidris s.r.l., Viale Gran Sasso 17, 20131 Milan, Italy.
Cappelletti
Graziella
G
Casagrande
Manolo
M
Perrino
Elena
E
Renzi
Luigi
L
Del Soldato
Piero
P
Sparatore
Anna
A
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006655:Histone Deacetylases / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014635:Valproic Acid / Q000737:chemistry
D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; C552757:N-hydroxy-5-(4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy)pentanamide; C552758:N-hydroxy-7-(4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy)heptanamide; D013876:Thiophenes; D014635:Valproic Acid; D006655:Histone Deacetylases