Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors

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DOI:10.1021/acsmedchemlett.3c00242
作者：Paul Bamborough*,?Chun-wa Chung,?Nicole C. Goodwin,?Darren J. Mitchell,?Christopher E. Neipp,?Alex Phillipou,?Alex Preston,?Rab K. Prinjha,?Peter E. Soden,?Robert J. Watson and Emmanuel H. Demont,?
文献类型：期刊论文
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American Chemical Society (ACS)

Abstract：The 1,3-dihydro-2H-benzo[d]azepin-2-ones are potent and ligand-efficient pan-BET bromodomain inhibitors. Here we describe the extension of this template to exploit a bivalent mode of action,

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