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. 2017 May 15;27(10):2225-2233.
doi: 10.1016/j.bmcl.2017.02.057. Epub 2017 Feb 24.

Methylpyrrole Inhibitors of BET Bromodomains


Methylpyrrole Inhibitors of BET Bromodomains

Lisa A Hasvold et al. Bioorg Med Chem Lett. .


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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