Orthogonal functionalisation of α-helix mimetics† †Electronic supplementary information (ESI) available: Additional binding data and fluorescence characterisation. Experimental procedures and characterisation of all new compounds. See DOI: 10.1039/c4ob00915k Click here for additional data file.

نویسندگان

  • Anna Barnard
  • Kérya Long
  • David J. Yeo
  • Jennifer A. Miles
  • Valeria Azzarito
  • George M. Burslem
  • Panchami Prabhakaran
  • Thomas A. Edwards
  • Andrew J. Wilson
چکیده

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.

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منابع مشابه

Enantioselective Narasaka–Heck cyclizations: synthesis of tetrasubstituted nitrogen-bearing stereocenters† †Electronic supplementary information (ESI) available: Experimental procedures and characterisation data for all compounds are provided. CCDC 1438659 and 1438660. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c6sc04466b Click here for additional data file. Click here for additional data file.

School of Chemistry, University of Bristol, B bris.ac.uk AstraZeneca, Alderley Park, Maccleseld, C AstraZeneca, Pepparedsleden 1, Mölndal, 4 † Electronic supplementary information ( and characterisation data for all compou 1438660. For ESI and crystallographic dat DOI: 10.1039/c6sc04466b ‡ These authors contributed equally. § Author to whom correspondence shou structures of 3b and Pd[(Sa,S)-L-...

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Recognition of extended linear and cyclised polyketide mimics by a type II acyl carrier protein† †Electronic supplementary information (ESI) available: Detailed experimental procedures and characterisation data for all new compounds, additional spectra and structural statistics for derivatised ACP three-dimensional structures. See DOI: 10.1039/c5sc03864b Click here for additional data file.

School of Chemistry, University of Bristol, E-mail: [email protected]; chris.wil † Electronic supplementary information procedures and characterisation data for and structural statistics for derivatised A DOI: 10.1039/c5sc03864b ‡ Current address: CAS Key Laboratory Systems, Wuhan Institute of Physics and of Sciences, Wuhan, Hubei Province 4300 § Current address: Fyeld Business & Res CM...

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عنوان ژورنال:

دوره 12  شماره 

صفحات  -

تاریخ انتشار 2014