Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
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Huang H, Hutta DA, Hu H, DesJarlais RL, Schubert C, Petrounia IP, Chaikin MA, Manthey CL, Player MR
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2355-61. doi: 10.1016/j.bmcl.2008.02.070. Epub 2008 Mar 4.
- PubMed ID
- 18342505 [ View in PubMed]
- Abstract
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%.