5443-23-2Relevant academic research and scientific papers
A novel protocol for the one-pot borylation/Suzuki reaction provides easy access to hinge-binding groups for kinase inhibitors
Hooper,Zambon,Springer
, p. 963 - 969 (2016/01/15)
The one-pot borylation/Suzuki reaction is a very efficient means of accessing cross-coupling products of two aryl-halide partners that generally requires the use of specific catalysts or ligands and/or relatively long reaction times. This new microwave-assisted method provides a quick one-pot borylation/Suzuki reaction protocol that we applied to the synthesis of various bi- or poly-aryl scaffolds, including a variety of aryl and heteroaryl ring systems and the core frameworks of kinase inhibitors vemurafenib and GDC-0879.
4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2)
Olsson, Henric,Sjoe, Peter,Ersoy, Oguz,Kristoffersson, Anna,Larsson, Joakim,Norden, Bo
scheme or table, p. 4738 - 4740 (2010/10/02)
A class of inhibitors of mitogen activated protein kinase-activated kinase 2 (MK2) was discovered via high-throughput screening. This compound class demonstrates activity against the enzyme with sub-μM IC50 values, and suppresses LPS-induced TN
