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Published on: June 23, 2019
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors
Matthew O Duffey1, Ruth Adams, Christopher Blackburn
1Millennium Pharmaceuticals, Inc., Oncology, Medicinal Chemistry, 40 Landsdowne St., Cambridge, MA 02139, United States. matthew.duffey@mpi.com
Bioorganic & Medicinal Chemistry Letters
|July 17, 2010
Abstract:
The discovery of novel pyrazoline derivatives as B-Raf (V600E) inhibitors is described in this report. Chemical modification of the pyrazoline scaffold led to the development of SAR and identified potent and selective inhibitors of B-Raf (V600E). Determination of the pharmacokinetic properties of selected inhibitors is also reported.
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