title: Enantioselective total synthesis of pladienolide B: a potent spliceosome inhibitor.
abstract: An enantioselective and convergent total synthesis of pladienolide B (1) is described. Pladienolide B binds to the SF3b complex of a spliceosome and inhibits mRNA splicing activity. The synthesis features an epoxide opening reaction, an asymmetric reduction of a β-keto ester, and a cross metathesis strategy for the side chain synthesis.
authors.affiliation: Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, USA. akghosh@purdue.edu
authors.forename: Arun K
authors.initials: AK
authors.lastname: Ghosh
authors.forename: David D
authors.initials: DD
authors.lastname: Anderson
mesh_terms: D004852:Epoxy Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D017381:Spliceosomes / Q000187:drug effects*; D013237:Stereoisomerism
chemical_list: D004852:Epoxy Compounds; D018942:Macrolides; C522342:pladienolide B