Discovery of thienopyridines as Src-family selective Lck inhibitors.
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.
Abbott
Lily
L
Abbott Bioresearch Center, 100 Research Drive, Worcester, MA 01605-5314, USA.
Betschmann
Patrick
P
Burchat
Andrew
A
Calderwood
David J
DJ
Davis
Heather
H
Hrnciar
Peter
P
Hirst
Gavin C
GC
Li
Biqin
B
Morytko
Michael
M
Mullen
Kelly
K
Yang
Bryant
B
D001665:Binding Sites; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors
D011725:Pyridines; C446540:thienopyridine; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck); D019061:src-Family Kinases