On May 31, 2020, Yin, Yuan; Chen, Cheng-Juan; Yu, Ru-Nan; Shu, Lei; Wang, Zhi-Jian; Zhang, Tian-Tai; Zhang, Da-Yong published an article.Synthetic Route of 4433-40-3 The title of the article was Novel 1H-pyrazolo[3,4-d]pyrimidin-6-amino derivatives as potent selective Janus kinase 3 (JAK3) inhibitors. Evaluation of their improved effect for the treatment of rheumatoid arthritis. And the article contained the following:
Selective JAK3 inhibitors have been shown to have a potential benefit in the treatment of autoimmune disorders. Here we report the identification of a series of pyrazolopyrimidine derivatives as potent JAK3 inhibitors that exploit a unique cysteine (Cys909) residue in JAK3. Most of these compounds (13k, 13n and 13 t), displayed stronger anti-JAK3 kinase activity and selectivity than tofacitinib. Furthermore, the most active inhibitor 13t (IC50 = 0.1 nM), also exhibited favorable selectivity for JAK3 in a panel of 9 kinases which contain the same cysteine. In a series of cytokine-stimulated cellular anal., compound 13 t, could potently block the JAK3-STAT signaling pathway. Further biol. studies, including cellular antiproliferative activity assays and a rat adjuvant-induced arthritis model for in vivo evaluation, also indicated its efficacy and low toxicity in the treatment of rheumatoid arthritis. The results of these exptl. explorations suggested that 13t is a promising lead compound for the development of selective JAK3 inhibitor with therapeutic potential in rheumatoid arthritis. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Synthetic Route of 4433-40-3
The Article related to pyrazolo pyrimidin amino derivative preparation jak3 inhibitor rheumatoid arthritis, 4-d]pyrimidin, autoimmune diseases, jak3 inhibitors, pyrazolo[3, rheumatoid arthritis and other aspects.Synthetic Route of 4433-40-3
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia