Discovery of novel FMS kinase inhibitors as anti-inflammatory agents

Carl R Illig; Jinsheng Chen; Mark J Wall; Kenneth J Wilson; Shelley K Ballentine; M Jonathan Rudolph; Renee L DesJarlais; Yanmin Chen; Carsten Schubert; Ioanna Petrounia; Carl S Crysler; Christopher J Molloy; Margery A Chaikin; Carl L Manthey; Mark R Player; Bruce E Tomczuk; Sanath K Meegalla

doi:10.1016/j.bmcl.2008.01.059

Discovery of novel FMS kinase inhibitors as anti-inflammatory agents

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1642-8. doi: 10.1016/j.bmcl.2008.01.059. Epub 2008 Jan 19.

Authors

Carl R Illig¹, Jinsheng Chen, Mark J Wall, Kenneth J Wilson, Shelley K Ballentine, M Jonathan Rudolph, Renee L DesJarlais, Yanmin Chen, Carsten Schubert, Ioanna Petrounia, Carl S Crysler, Christopher J Molloy, Margery A Chaikin, Carl L Manthey, Mark R Player, Bruce E Tomczuk, Sanath K Meegalla

Affiliation

¹ Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, Spring House, PA 19477, USA.

PMID: 18242992
DOI: 10.1016/j.bmcl.2008.01.059

Abstract

The optimization of the arylamide lead 2 resulted in identification of a highly potent series of 2,4-disubstituted arylamides. Compound 8 (FMS kinase IC(50)=0.0008 microM) served as a proof-of-concept candidate in a collagen-induced model of arthritis in mice.

MeSH terms

Animals
Anti-Inflammatory Agents / chemistry*
Anti-Inflammatory Agents / pharmacology*
Arthritis / chemically induced
Arthritis / drug therapy
Collagen
Dose-Response Relationship, Drug
Mice
Models, Molecular
Molecular Structure
Receptor, Macrophage Colony-Stimulating Factor / antagonists & inhibitors*
Structure-Activity Relationship
Time Factors

Substances

Anti-Inflammatory Agents
Collagen
Receptor, Macrophage Colony-Stimulating Factor