Total synthesis of (+)-A83586C, (+)- kettapeptin and (+)-azinothricin: powerful new inhibitors of β-catenin/TCF4- and E2F-mediated gene transcription

Hale, K.Manaviazar, S.George, J.2011-12-072011-12-072010Chemical Communications, 2010; 46(23):4021-40421359-73451364-548Xhttp://hdl.handle.net/2440/68553Herein we describe our asymmetric total syntheses of (+)-A83586C, (+)-kettapeptin and (+)-azinothricin. We also demonstrate that molecules of this class powerfully inhibit β-catenin/TCF4- and E2F-mediated gene transcription within malignant human colon cancer cells at low drug concentrations.enThis journal is copyright The Royal Society of Chemistry 2010Cell Line, TumorHumansColonic NeoplasmsDepsipeptidesPeptidesTranscription FactorsTranscription, GeneticE2F Transcription Factorsbeta CateninBasic Helix-Loop-Helix Leucine Zipper Transcription FactorsTranscription Factor 4Total synthesis of (+)-A83586C, (+)- kettapeptin and (+)-azinothricin: powerful new inhibitors of β-catenin/TCF4- and E2F-mediated gene transcriptionTotal synthesis of (+) - A83586C, (+)- kettapeptin and (+)- azinothricin: powerful new inhibitors of beta-catenin/TCF4- and E2F-mediated gene transcriptionJournal article002011255710.1039/C000603C0002783649000012-s2.0-7795320240827834George, J. [0000-0002-7330-2160]