title: Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
abstract: A series of benzimidazole based HDAC inhibitors have been rationally designed, synthesized and screened. The SAR of this new chemotype is described. The lead compound, 11e, showed strong activity in several cellular assays and demonstrated in vivo efficacy in mouse xenograft pancreatic cancer models.
authors.affiliation: Translational Drug Development, Inc, 13208 E Shea Boulevard, Suite 100, Scottsdale, AZ 85259,USA. twang@td2inc.com
authors.forename: Tong
authors.initials: T
authors.lastname: Wang
authors.forename: Mario
authors.initials: M
authors.lastname: Sepulveda
authors.forename: Paul
authors.initials: P
authors.lastname: Gonzales
authors.forename: Stephen
authors.initials: S
authors.lastname: Gately
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010179:Pancreas / Q000187:drug effects / Q000201:enzymology; D010190:Pancreatic Neoplasms / Q000188:drug therapy / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D056572:Histone Deacetylase Inhibitors; C031000:benzimidazole; D006655:Histone Deacetylases
keywords: Anticancer agents; Benzimidazole; HDAC inhibitors; Structure–activity relationship