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, 27 (10), 2225-2233

Methylpyrrole Inhibitors of BET Bromodomains

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Methylpyrrole Inhibitors of BET Bromodomains

Lisa A Hasvold et al. Bioorg Med Chem Lett.

Abstract

An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further modifications to the methylpyrrole core provided compounds with improved properties and enhanced activity in a mouse model of multiple myeloma.

Keywords: BET proteins; Bromodomain; Fragment screening.

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