Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3)

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 5; pp. 1250 - 1253
• Main Authors: Clark, Michael P., George, Kelly M., Bookland, Roger G., Chen, Jack, Laughlin, Steven K., Thakur, Kumar D., Lee, Wenlin, Davis, Jan R., Cabrera, Ed J., Brugel, Todd A., VanRens, John C., Laufersweiler, Matthew J., Maier, Jennifer A., Sabat, Mark P., Golebiowski, Adam, Easwaran, Vijay, Webster, Mark E., De, Biswanath, Zhang, George
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.03.2007; Elsevier
• Subjects: Autoimmune Diseases - drug therapy; Biological and medical sciences; Cell Line, Tumor; Cell Proliferation - drug effects; Cytokines; Humans; Immunity - drug effects; Immunomodulators; JAK3; Janus Kinase; Janus Kinase 2 - antagonists & inhibitors; Janus Kinase 3 - antagonists & inhibitors; Medical sciences; Pharmacology. Drug treatments; Pyrimidines - chemical synthesis; Pyrimidines - pharmacology; Pyrroles - chemical synthesis; Pyrroles - pharmacology; Pyrrolopyrimidine; Structure-Activity Relationship; Tyrosine kinases; Tyrosine kinases; Pyrrolopyrimidine; Janus Kinase; Cytokines; JAK3; Enzyme; Transferases; Cytokine; Alcohol; In vitro; Immunomodulator; Signal transduction; Imidazopyridine derivatives; Cell line; Structure activity relation; Bicyclic compound; Inhibitor; Piperazine derivatives; Chemical synthesis; Protein-tyrosine kinase
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.12.018

A new class of bicyclic pyrrolopyrimidine-based Janus kinase 3 (JAK-3) inhibitors are described. Many of these inhibitors showed low nanomolar activity against JAK-3.