Discovery of thienopyridines as Src-family selective Lck inhibitors

Lily Abbott; Patrick Betschmann; Andrew Burchat; David J Calderwood; Heather Davis; Peter Hrnciar; Gavin C Hirst; Biqin Li; Michael Morytko; Kelly Mullen; Bryant Yang

doi:10.1016/j.bmcl.2006.12.035

Discovery of thienopyridines as Src-family selective Lck inhibitors

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1167-71. doi: 10.1016/j.bmcl.2006.12.035. Epub 2006 Dec 15.

Authors

Lily Abbott¹, Patrick Betschmann, Andrew Burchat, David J Calderwood, Heather Davis, Peter Hrnciar, Gavin C Hirst, Biqin Li, Michael Morytko, Kelly Mullen, Bryant Yang

Affiliation

¹ Abbott Bioresearch Center, 100 Research Drive, Worcester, MA 01605-5314, USA.

PMID: 17234410
DOI: 10.1016/j.bmcl.2006.12.035

Abstract

We describe the identification, SAR, and in vivo pharmacology of a new series of Src-family selective Lck inhibitors. These thienopyridines were designed based on a desire to access the unique residues in the extended hinge region of Lck.

MeSH terms

Binding Sites
Drug Design
Humans
Inhibitory Concentration 50
Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
Pyridines / chemistry*
Pyridines / pharmacology
Structure-Activity Relationship
src-Family Kinases / antagonists & inhibitors

Substances

Pyridines
thienopyridine
Lymphocyte Specific Protein Tyrosine Kinase p56(lck)
src-Family Kinases