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Issue 35, 2014
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Orthogonal functionalisation of α-helix mimetics

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Abstract

α-Helix mediated protein–protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using ‘click’ chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.

Graphical abstract: Orthogonal functionalisation of α-helix mimetics

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Supplementary files

Article information


Submitted
04 May 2014
Accepted
07 Jul 2014
First published
28 Jul 2014

This article is Open Access

Org. Biomol. Chem., 2014,12, 6794-6799
Article type
Communication
Author version available

Orthogonal functionalisation of α-helix mimetics

A. Barnard, K. Long, D. J. Yeo, J. A. Miles, V. Azzarito, G. M. Burslem, P. Prabhakaran, T. A. Edwards and A. J. Wilson, Org. Biomol. Chem., 2014, 12, 6794
DOI: 10.1039/C4OB00915K

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