title: Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs.
abstract: The synthesis of an isosteric analog of the natural product and HDAC inhibitor largazole is described. The sulfur atom in the thizaole ring of the natural product has been replaced with an oxygen atom, constituting an oxazole ring. The biochemical activity and cytotoxicity of this species is described.
authors.affiliation: Department of Chemistry, Colorado State University, Fort Collins, CO 80523, United States.
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Guerra-Bubb
authors.forename: Albert A
authors.initials: AA
authors.lastname: Bowers
authors.forename: William B
authors.initials: WB
authors.lastname: Smith
authors.forename: Ronald
authors.initials: R
authors.lastname: Paranal
authors.forename: Guillermina
authors.initials: G
authors.lastname: Estiu
authors.forename: Olaf
authors.initials: O
authors.lastname: Wiest
authors.forename: James E
authors.initials: JE
authors.lastname: Bradner
authors.forename: Robert M
authors.initials: RM
authors.lastname: Williams
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D047630:Depsipeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D062105:Molecular Docking Simulation; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D056572:Histone Deacetylase Inhibitors; D010080:Oxazoles; D013844:Thiazoles; C527895:largazole
keywords: Conformation; HDAC; Isostere; Largazole; Oxazole
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