1350712-69-4Relevant articles and documents
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors
Jaime-Figueroa, Saul,De Vicente, Javier,Hermann, Johannes,Jahangir, Alam,Jin, Sue,Kuglstatter, Andreas,Lynch, Stephen M.,Menke, John,Niu, Linghao,Patel, Vaishali,Shao, Ada,Soth, Michael,Vu, Minh Diem,Yee, Calvin
, p. 2522 - 2526 (2013/06/26)
We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold. The initial leads in this series, compounds 1a and 1h, showed promising potencies, but a lack of selectivity against other isoforms in the JAK family. Computational and crystallographic analysis suggested that the phenyl ether moiety possessed a favorable vector to achieve selectivity. Exploration of this vector resulted in the identification of 12b and 12d, as potent JAK3 inhibitors, demonstrating improved JAK family and kinase selectivity.
