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Methylpyrrole inhibitors of BET bromodomains

Lisa A. Hasvold,George S. Sheppard,Le Wang,Steven D. Fidanze,Dachun Liu,John K. Pratt,Robert A. Mantei,Carol K. Wada, Robbert Hubbard,Yu Shen,Xiaoyu Lin,Xiaoli Huang,Scott E. Warder,Denise Wilcox,Leiming Li,F. Greg Buchanan, Lauren Smithee,Daniel H. Albert,Terrance J. Magoc,Chang H. Park,Andrew M. Petros,Sanjay C. Panchal,Chaohong Sun,Peter Kovar,Nirupama B. Soni,Steven W. Elmore,Warren M. Kati,Keith F. McDaniel

Bioorganic & Medicinal Chemistry Letters（2017）

Cited 19|Views76
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Abstract
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.
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Key words
BET proteins,Bromodomain,Fragment screening
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