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Discovery of Benzotriazolo[4,3-<i>d</i>][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

25 Mar 2015

Abstract excerpt

Inhibition of the bromodomains of the BET family, of which BRD4 is a member, has been shown to decrease myc and interleukin (IL) 6 in vivo, markers that are of therapeutic relevance to cancer and inflammatory disease, respectively. Herein we report substituted benzo[b]isoxazolo[4,5-d]azepines and benzotriazolo[4,3-d][1,4]diazepines as fragment-derived novel inhibitors of the bromodomain of BRD4. Compounds from...

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PMID: 26985289
DOI: 10.1021/ml500411h

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