Abstract
Herein we describe our asymmetric total syntheses of (+)-A83586C, (+)-kettapeptin and (+)-azinothricin. We also demonstrate that molecules of this class powerfully inhibit beta-catenin/TCF4- and E2F-mediated gene transcription within malignant human colon cancer cells at low drug concentrations.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Basic Helix-Loop-Helix Leucine Zipper Transcription Factors / antagonists & inhibitors*
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Basic Helix-Loop-Helix Leucine Zipper Transcription Factors / metabolism
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Cell Line, Tumor
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Colonic Neoplasms / drug therapy*
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Colonic Neoplasms / genetics
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Colonic Neoplasms / metabolism
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Depsipeptides / chemical synthesis
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Depsipeptides / pharmacology*
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E2F Transcription Factors / genetics*
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E2F Transcription Factors / metabolism
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Humans
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Peptides / chemical synthesis
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Peptides / pharmacology*
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Transcription Factor 4
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Transcription Factors / antagonists & inhibitors*
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Transcription Factors / metabolism
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Transcription, Genetic / drug effects*
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beta Catenin / antagonists & inhibitors*
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beta Catenin / metabolism
Substances
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Basic Helix-Loop-Helix Leucine Zipper Transcription Factors
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Depsipeptides
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E2F Transcription Factors
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Peptides
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TCF4 protein, human
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Transcription Factor 4
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Transcription Factors
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beta Catenin
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kettapeptin
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azinothricin
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A 83586C