Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. 2008

Carl R Illig, and Jinsheng Chen, and Mark J Wall, and Kenneth J Wilson, and Shelley K Ballentine, and M Jonathan Rudolph, and Renee L DesJarlais, and Yanmin Chen, and Carsten Schubert, and Ioanna Petrounia, and Carl S Crysler, and Christopher J Molloy, and Margery A Chaikin, and Carl L Manthey, and Mark R Player, and Bruce E Tomczuk, and Sanath K Meegalla
Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, Spring House, PA 19477, USA.

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.

UI MeSH Term Description Entries
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D003094 Collagen A polypeptide substance comprising about one third of the total protein in mammalian organisms. It is the main constituent of SKIN; CONNECTIVE TISSUE; and the organic substance of bones (BONE AND BONES) and teeth (TOOTH). Avicon,Avitene,Collagen Felt,Collagen Fleece,Collagenfleece,Collastat,Dermodress,Microfibril Collagen Hemostat,Pangen,Zyderm,alpha-Collagen,Collagen Hemostat, Microfibril,alpha Collagen
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents
D001168 Arthritis Acute or chronic inflammation of JOINTS. Oligoarthritis,Polyarthritis,Arthritides,Oligoarthritides,Polyarthritides
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D016186 Receptor, Macrophage Colony-Stimulating Factor A receptor for MACROPHAGE COLONY-STIMULATING FACTOR encoded by the c-fms proto-oncogene (GENES, FMS). It contains an intrinsic protein-tyrosine kinase activity. When activated the receptor undergoes autophosphorylation, phosphorylation of down-stream signaling molecules and rapid down-regulation. Antigens, CD115,CD115 Antigens,CSF-1 Receptor,M-CSF Receptor,Macrophage Colony-Stimulating Factor Receptor,Proto-Oncogene Protein fms,Receptor, CSF-1,c-fms Protein,fms Proto-Oncogene Protein,CD115 Antigen,M-CSF Receptors,Macrophage Colony-Stimulating Factor Receptors,Receptors, CSF-1,Receptors, M-CSF,Receptors, Macrophage Colony-Stimulating Factor,Antigen, CD115,CSF-1 Receptors,M CSF Receptor,Macrophage Colony Stimulating Factor Receptor,Macrophage Colony Stimulating Factor Receptors,Proto-Oncogene Protein, fms,Receptor, CSF 1,Receptor, M-CSF,Receptor, Macrophage Colony Stimulating Factor,Receptors, CSF 1,Receptors, M CSF,Receptors, Macrophage Colony Stimulating Factor,c fms Protein,fms Proto Oncogene Protein

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