Discovery of 2-(alpha-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS

Christopher J Burns; Michael F Harte; Xianyong Bu; Emmanuelle Fantino; Marilena Giarrusso; Max Joffe; Margarita Kurek; Fiona S Legge; Pasquale Razzino; Stephen Su; Herbert Treutlein; Soo San Wan; Jun Zeng; Andrew F Wilks

doi:10.1016/j.bmcl.2008.12.073

Discovery of 2-(alpha-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1206-9. doi: 10.1016/j.bmcl.2008.12.073. Epub 2008 Dec 25.

Authors

Christopher J Burns¹, Michael F Harte, Xianyong Bu, Emmanuelle Fantino, Marilena Giarrusso, Max Joffe, Margarita Kurek, Fiona S Legge, Pasquale Razzino, Stephen Su, Herbert Treutlein, Soo San Wan, Jun Zeng, Andrew F Wilks

Affiliation

¹ Cytopia Research Pty Ltd, 576 Swan Street, Richmond, VIC. 3121, Australia.

PMID: 19128971
DOI: 10.1016/j.bmcl.2008.12.073

Abstract

A series of 2-(alpha-methylbenzylamino) pyrazines have shown to be potent inhibitors of the FMS tyrosine receptor kinase. Details of SAR studies, modeling and synthesis of compounds within this series are reported.

MeSH terms

Combinatorial Chemistry Techniques
Drug Design
Models, Molecular*
Molecular Structure
Pyrazines / chemical synthesis*
Pyrazines / chemistry
Pyrazines / pharmacology*
Receptor, Macrophage Colony-Stimulating Factor / antagonists & inhibitors*
Stereoisomerism
Structure-Activity Relationship

Substances

Pyrazines
Receptor, Macrophage Colony-Stimulating Factor