Discovery of 1-Methyl-1H-imidazole Derivatives as Potent Jak2 Inhibitors was written by Su, Qibin;Ioannidis, Stephanos;Chuaqui, Claudio;Almeida, Lynsie;Alimzhanov, Marat;Bebernitz, Geraldine;Bell, Kirsten;Block, Michael;Howard, Tina;Huang, Shan;Huszar, Dennis;Read, Jon A.;Rivard Costa, Caroline;Shi, Jie;Su, Mei;Ye, Minwei;Zinda, Michael. And the article was included in Journal of Medicinal Chemistry in 2014.Related Products of 938443-20-0 This article mentions the following:
Structure based design, synthesis, and biol. evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clin. candidate AZD1480 (I), optimization of the series led to the discovery of compound II, a potent, orally bioavailable Jak2 inhibitor. Compound II displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound II demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range. In the experiment, the researchers used many compounds, for example, 2,4,7-Trichloropyrido[2,3-d]pyrimidine (cas: 938443-20-0Related Products of 938443-20-0).
2,4,7-Trichloropyrido[2,3-d]pyrimidine (cas: 938443-20-0) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Related Products of 938443-20-0
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia