期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 10, 页码 2225-2233出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.02.057
关键词
BET proteins; Bromodomain; Fragment screening
资金
- Industrial Macromolecular Crystallography Association through Hauptman-Woodward Medical Research Institute
- DOE Office of Science [DE-AC02-06CH11357]
- AbbVie
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. (C) 2017 Elsevier Ltd. All rights reserved.
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