title: N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
abstract: With the aim to discover novel HDAC inhibitors with high potency and good safety profiles, we have designed a small library based on a N-hydroxy-(4-oxime)-cinnamide scaffold. We describe the synthesis of these novel compounds and some preliminary in vitro cytotoxic activity on three tumor cell lines, NB4, H460 and HCT116, as well as their inhibitory activity against class I, II and IV HDAC. Several 4-oxime derivatives demonstrated a promising inhibitory activity on HDAC6 and HDAC8 coupled to a good selectivity profile.
authors.affiliation: R&D Sigma-Tau SpA, Pomezia, Italy. giuseppe.giannini@sigma-tau.it
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Giannini
authors.forename: Mauro
authors.initials: M
authors.lastname: Marzi
authors.forename: Riccardo
authors.initials: R
authors.lastname: Pezzi
authors.forename: Tiziana
authors.initials: T
authors.lastname: Brunetti
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Battistuzzi
authors.forename: Maria Di
authors.initials: MD
authors.lastname: Marzo
authors.forename: Walter
authors.initials: W
authors.lastname: Cabri
authors.forename: Loredana
authors.initials: L
authors.lastname: Vesci
authors.forename: Claudio
authors.initials: C
authors.lastname: Pisano
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D002934:Cinnamates / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000145:classification / Q000378:metabolism; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000145:classification / Q000378:metabolism; D011485:Protein Binding / Q000502:physiology
chemical_list: D000970:Antineoplastic Agents; D002934:Cinnamates; D056572:Histone Deacetylase Inhibitors; D007527:Isoenzymes; D006655:Histone Deacetylases