Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains

Duncan A. Hay; Catherine M. Rogers; Oleg Fedorov; Cynthia Tallant; Sarah Martin; Octovia P. Monteiro; Susanne Müller; Stefan Knapp; Christopher J. Schofield; Paul E. Brennan

doi:10.1039/C5MD00152H

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains†

Duncan A. Hay,‡^ab Catherine M. Rogers,‡^bc Oleg Fedorov,^bc Cynthia Tallant,^bc Sarah Martin,^bc Octovia P. Monteiro,^bc Susanne Müller,^bc Stefan Knapp,^bc Christopher J. Schofield^a and Paul E. Brennan*^bc

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* Corresponding authors

^a Department of Chemistry, University of Oxford, South Parks Road, Oxford OX1 3TA, UK

^b Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford, UK
E-mail: paul.brennan@sgc.ox.ac.uk

^c Target Discovery Institute, University of Oxford, NDM Research Building, Roosevelt Drive, Oxford, UK

Abstract

Emerging evidence suggests bromodomain-containing proteins 7 and 9 (BRD7 and BRD9) have roles in the regulation of human transcription and disease including cancer. We describe potent and selective inhibitors of the BRD7 and BRD9 bromodomains intended for use as tools to elucidate the biological roles of BRD7 and BRD9 in healthy and diseased cells.

MedChemComm

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains†

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Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains

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