《Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma》 was written by Chen, Yun; Bai, Gang; Ning, Yi; Cai, Shi; Zhang, Tao; Song, Peiran; Zhou, Jinpei; Duan, Wenhu; Ding, Jian; Xie, Hua; Zhang, Huibin. Quality Control of 3-(Trifluoromethyl)-1H-pyrazole And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
The design, synthesis and structure-activity relationships of imidazo[1,2-b]pyridazines I [R = 2-aminoethyl, 3-amino-piperidin-1-yl, piperazin-1-yl, etc.; R1 = CF2, CF3, CN, etc.; R2 =Me, Et, iPr, etc.; R3 = H, Me] as potent IRAK4 inhibitors was reported. The representative compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] exhibited excellent IRAK4 potency (IRAK4 IC50 = 1.3 nM) and favorable kinase selectivity profile. It demonstrated cellular selectivity for activated B cell-like (ABC) subtype DLBCL with MYD88 L265P mutation in cytotoxicity assay. The kinase inhibitory efficiency of compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] was further validated by western blot anal. of phosphorylation of IRAK4 and downstream signaling in OCI-LY10 and TMD8 cells. Besides, combination of compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] and BTK inhibitor ibrutinib synergistically reduced the viability of TMD8 cells. These results indicated that compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] could be a promising IRAK4 inhibitor for the treatment of mutant MYD88 DLBCL. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Quality Control of 3-(Trifluoromethyl)-1H-pyrazole)
3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Quality Control of 3-(Trifluoromethyl)-1H-pyrazole
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics