Issue 23, 2010
From the journal:

Chemical Communications

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

Karl J. Hale,*a   Soraya Manaviazara  and  Jonathan Georgeb  

* Corresponding authors

a The School of Chemistry and Chemical Engineering, and the Centre for Cancer Research and Cell Biology (CCRCB), Queen 's University Belfast, Stranmillis Road, Belfast, Northern Ireland, UK
E-mail: k.j.hale@qub.ac.uk, s.manaviazar@qub.ac.uk
Fax: +44-(0)289097-4579
Tel: +44-(0)289097-5525

b Department of Chemistry, University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, Oxford, UK

Abstract

Herein 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.

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

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Article information

DOI
https://doi.org/10.1039/C000603C
Article type
Feature Article
Submitted
11 Jan 2010
Accepted
04 Mar 2010
First published
19 Apr 2010

Chem. Commun., 2010,46, 4021-4042

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

K. J. Hale, S. Manaviazar and J. George, Chem. Commun., 2010, 46, 4021 DOI: 10.1039/C000603C

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