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.Formula: C4H5N3O2 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, 1-Methyl-4-nitroimidazole (cas: 3034-41-1Formula: C4H5N3O2).
1-Methyl-4-nitroimidazole (cas: 3034-41-1) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole is incorporated into many important biological compounds. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Histidine is present in many proteins and enzymes, e.g. by binding metal cofactors, as seen in hemoglobin.Formula: C4H5N3O2
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem