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

Michael P Clark; Kelly M George; Roger G Bookland; Jack Chen; Steven K Laughlin; Kumar D Thakur; Wenlin Lee; Jan R Davis; Ed J Cabrera; Todd A Brugel; John C VanRens; Matthew J Laufersweiler; Jennifer A Maier; Mark P Sabat; Adam Golebiowski; Vijay Easwaran; Mark E Webster; Biswanath De; George Zhang

doi:10.1016/j.bmcl.2006.12.018

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

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1250-3. doi: 10.1016/j.bmcl.2006.12.018. Epub 2006 Dec 9.

Affiliation

¹ Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason, OH 45040, USA. mclark@metastatix.com

PMID: 17189692
DOI: 10.1016/j.bmcl.2006.12.018

Abstract

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.

MeSH terms

Autoimmune Diseases / drug therapy
Cell Line, Tumor
Cell Proliferation / drug effects
Humans
Immunity / drug effects
Janus Kinase 2 / antagonists & inhibitors
Janus Kinase 3 / antagonists & inhibitors*
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology
Pyrroles / chemical synthesis*
Pyrroles / pharmacology
Structure-Activity Relationship

Substances

Pyrimidines
Pyrroles
Janus Kinase 2
Janus Kinase 3