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, 58 (15), 6151-78

Structure-Based Optimization of Naphthyridones Into Potent ATAD2 Bromodomain Inhibitors

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Structure-Based Optimization of Naphthyridones Into Potent ATAD2 Bromodomain Inhibitors

Paul Bamborough et al. J Med Chem.

Abstract

ATAD2 is a bromodomain-containing protein whose overexpression is linked to poor outcomes in a number of different cancer types. To date, no potent and selective inhibitors of the bromodomain have been reported. This article describes the structure-based optimization of a series of naphthyridones from micromolar leads with no selectivity over the BET bromodomains to inhibitors with sub-100 nM ATAD2 potency and 100-fold BET selectivity.

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