title: Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors.
abstract: New histone deacetylase inhibitors have been synthesized and evaluated for their activity against non-small lung cancer cell line H661. These compounds have been designed with diversely substituted 1,4-benzodiazepine-2,5-dione moieties as cyclic peptide mimic cap structures, and a hydroxamate side chain. Biological evaluations demonstrated that benzodiazepine-based HDACi bearing an aromatic substituent at the N1 position exhibited promising antiproliferative and HDAC-inhibitory activities.
authors.affiliation: Université de Poitiers, CNRS UMR 6514, SRSN, 40 Avenue du Recteur Pineau, 86022, Poitiers, France.
authors.forename: Lynda
authors.initials: L
authors.lastname: Loudni
authors.forename: Joëlle
authors.initials: J
authors.lastname: Roche
authors.forename: Vincent
authors.initials: V
authors.lastname: Potiron
authors.forename: Jonathan
authors.initials: J
authors.lastname: Clarhaut
authors.forename: Christian
authors.initials: C
authors.lastname: Bachmann
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Gesson
authors.forename: Isabelle
authors.initials: I
authors.lastname: Tranoy-Opalinski
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D050759:Cyclin-Dependent Kinase Inhibitor p21 / Q000737:chemistry; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000737:chemistry; D006657:Histones / Q000737:chemistry; D006801:Humans; D008956:Models, Chemical; D008968:Molecular Conformation; D011487:Protein Conformation; D014404:Tubulin / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; C493956:CDKN1A protein, human; D050759:Cyclin-Dependent Kinase Inhibitor p21; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006657:Histones; D014404:Tubulin; D001569:Benzodiazepines; D006655:Histone Deacetylases; C468549:Bz-423