title: Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
abstract: We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors. A series of 5,11-dihydrodibenzo[b,e]azepine-6-ones alkylated on the amide nitrogen with an alkyl chain bearing an hydroxamic acids moiety at the end, has been designed (based upon the general motif for HDAC inhibitors), synthesized and tested. This allowed us to identify a new series of submicromolar HDAC inhibitors, which showed antiproliferative activity on HCT-116 colon carcinoma cells.
authors.affiliation: Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia, Rome, Italy.
authors.forename: Mario
authors.initials: M
authors.lastname: Bigioni
authors.forename: Alessandro
authors.initials: A
authors.lastname: Ettorre
authors.forename: Patrizia
authors.initials: P
authors.lastname: Felicetti
authors.forename: Sandro
authors.initials: S
authors.lastname: Mauro
authors.forename: Cristina
authors.initials: C
authors.lastname: Rossi
authors.forename: Carlo Alberto
authors.initials: CA
authors.lastname: Maggi
authors.forename: Elena
authors.initials: E
authors.lastname: Marastoni
authors.forename: Monica
authors.initials: M
authors.lastname: Binaschi
authors.forename: Massimo
authors.initials: M
authors.lastname: Parlani
authors.forename: Daniela
authors.initials: D
authors.lastname: Fattori
mesh_terms: D001381:Azepines / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D001381:Azepines; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases