Issue 35, 2014

Orthogonal functionalisation of α-helix mimetics


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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Article information

Article type
04 May 2014
07 Jul 2014
First published
28 Jul 2014
This article is Open Access
Creative Commons BY license

Org. Biomol. Chem., 2014,12, 6794-6799

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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