Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 15, Pages 6151-6178Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b00773
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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 naphth-yridones 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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