National Center for
3BEA: Cfms Tyrosine Kinase (tie2 Kid) In Complex With A Pyrimidinopyridone Inhibitor
Bioorg. Med. Chem. Lett. (2008) 18 p.2355-2361
A series of pyrimidinopyridones has been designed, synthesized and shown to be potent and selective inhibitors of the FMS tyrosine kinase. Introduction of an amide substituent at the 6-position of the pyridone core resulted in a significant potency increase. Compound 24 effectively inhibited in vivo LPS-induced TNF in mice greater than 80%.