The structure based design of dual HDAC/BET inhibitors as novel epigenetic probesElectronic supplementary information (ESI) available. See DOI: 10.1039/c3md00285c

Herein we describe the design and synthesis of a dual active histone deacetylase (HDAC)/bromodomain and extra terminal (BET) small molecule tool inhibitor, DUAL946 ( 1 ). Exploiting our extensive epigenetic toolbox, we achieved the functionalisation of a BET active tetrahydroquinoline (THQ) core, wi...

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Hauptverfasser: Atkinson, Stephen J, Soden, Peter E, Angell, Davina C, Bantscheff, Marcus, Chung, Chun-wa, Giblin, Kathryn A, Smithers, Nicholas, Furze, Rebecca C, Gordon, Laurie, Drewes, Gerard, Rioja, Inmaculada, Witherington, Jason, Parr, Nigel J, Prinjha, Rab K
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Sprache:eng
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