Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton’s tyrosine kinase was written by Zhang, Dandan;Xu, Guiqing;Zhao, Jie;Wang, Yue;Wu, Xiaofang;He, Xing;Li, Wei;Zhang, Shuting;Yang, Shouning;Ma, Chunhua;Jiang, Yuqin;Ding, Qingjie. And the article was included in European Journal of Medicinal Chemistry in 2021.Related Products of 54916-28-8 This article mentions the following:
BTK (Bruton’s tyrosine kinase) inhibitors are the most promising drugs for the treatment of hematol. tumors. A high selectivity of BTK inhibitors ensures reduced side effects from off-targeting. Accordingly, here, based on Zanubrutinib, we designed and synthesized a new range of I, II and III. as novel BTK inhibitors that retained the amide group for improved selectivity. These compounds revealed potent inhibitory activity against BTK in vitro. Remarkably, compounds I [R1 = acryloyl, R2 = R3 = H; m = 1, n = 2] (IC50 5.2 nM) and I [R1 = but-2-ynoyl, R2 = R3 = H; m = 1, n = 2] (IC50 4.9 nM) possessed the highest kinase selectivity. Both of these effectively inhibited the auto-phosphorylation of BTK, blocked the cell cycle in G0/G1 phase, and induced apoptosis in the TMD8 cells. In a TMD8 cells xenograft model, a twice-daily dose of compound I [R1 = acryloyl, R2 = R3 = H; m = 1, n = 2] at 25 mg/kg and a thrice-daily dose of compound I [R1 = but-2-ynoyl, R2 = R3 = H; m = 1, n = 2] at 15 mg/kg significantly suppressed the tumor growth without obvious toxicity. Collectively, I [R1 = acryloyl, R2 = R3 = H; m = 1, n = 2] and I [R1 = but-2-ynoyl, R2 = R3 = H; m = 1, n = 2] are the potential selective BTK inhibitors that can be developed further. In the experiment, the researchers used many compounds, for example, 1-(4-(4-Methoxyphenoxy)phenyl)ethanone (cas: 54916-28-8Related Products of 54916-28-8).
1-(4-(4-Methoxyphenoxy)phenyl)ethanone (cas: 54916-28-8) belongs to ethers. Ether is less polar than esters, alcohols or amines because of the oxygen atom that is unable to participate in hydrogen bonding due to the presence of bulky alkyl groups on both sides of the oxygen atom. Ethyl ether is an excellent solvent for extractions and for a wide variety of chemical reactions. It is also used as a volatile starting fluid for diesel engines and gasoline engines in cold weather. Dimethyl ether is used as a spray propellant and refrigerant. Methyl t-butyl ether (MTBE) is a gasoline additive that boosts the octane number and reduces the amount of nitrogen-oxide pollutants in the exhaust. The ethers of ethylene glycol are used as solvents and plasticizers.Related Products of 54916-28-8
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem