In this section, you can access to the latest technical information related to the FUTURE project topic.

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors

A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 while maintaining good selectivity against JAK2 and Tyk2. Translation to in vivo efficacy was observed in a murine model of chronic inflammation. X-ray co-crystal structure determination confirmed the presumed inhibitor binding orientation in JAK3. Efforts to reduce hERG channel inhibition will be described.

» Author: John Hynes, Hong Wu, James Kempson, James J.-W. Duan, Zhonghui Lu, Bin Jiang, Sylwia Stachura, John S. Tokarski, John S. Sack, Javed A. Khan, Jonathan S. Lippy, Rosemary F. Zhang, Sidney Pitt, Guoxiang Shen, Kate Gillooly, K

» Reference: Bioorganic & Medicinal Chemistry Letters, Volume 27, Issue 14

» Publication Date: 15/07/2017

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