BRD4 Structure–Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536

[Image: see text] A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities. Particularly, replacement of the cyclopentyl group with a 3-bromobenzyl moiety afforded the most potent BRD4 inhibitor o...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: Chen, Lijia, Yap, Jeremy L., Yoshioka, Makoto, Lanning, Maryanna E., Fountain, Rachel N., Raje, Mithun, Scheenstra, Jacob A., Strovel, Jeffrey W., Fletcher, Steven
Format: Artigo
Language:Inglês
Published: American Chemical Society 2015
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4499818/
https://ncbi.nlm.nih.gov/pubmed/26191363
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00084
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