title: New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
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.
authors.affiliation: Sulfidris s.r.l., Viale Gran Sasso 17, 20131 Milan, Italy.
authors.forename: Valerio
authors.initials: V
authors.lastname: Tazzari
authors.forename: Graziella
authors.initials: G
authors.lastname: Cappelletti
authors.forename: Manolo
authors.initials: M
authors.lastname: Casagrande
authors.forename: Elena
authors.initials: E
authors.lastname: Perrino
authors.forename: Luigi
authors.initials: L
authors.lastname: Renzi
authors.forename: Piero
authors.initials: P
authors.lastname: Del Soldato
authors.forename: Anna
authors.initials: A
authors.lastname: Sparatore
mesh_terms: 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
chemical_list: 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