Application In Synthesis of 1-MethylpyrazoleOn June 9, 2022, Rong, Deqin; Zhou, Kaixin; Fang, Wei; Yang, Hong; Zhang, Yi; Shi, Qiongyu; Huang, Yuting; Li, Jiayi; Dong, Hui; Li, Lanlan; Ding, Jian; Huang, Xun; Wang, Yuanxiang published an article in Journal of Medicinal Chemistry. The article was 《Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5》. The article mentions the following:
PRMT5 is a major type II protein arginine methyltransferase and plays important roles in diverse cellular processes. Overexpression of PRMT5 is implicated in various types of cancer. Many efforts have been made to develop potent and selective PRMT5 inhibitors, the most potent of which is usually derived from nucleoside structures. Here, we designed a novel series of non-nucleoside PRMT5 inhibitors through the structure-aided drug design approach. SAR exploration and metabolic stability optimization led to the discovery of compound 41 as a potent PRMT5 inhibitor with good selectivity. Addnl., compound 41 exerted antiproliferative effects against A375 cells by inducing apoptosis and potently inhibited the methyltransferase activity of PRMT5 in cells. Moreover, it showed attractive pharmacokinetic properties and markedly suppressed the tumor growth in an A375 tumor xenograft model. These results clearly indicate that 41 is a highly potent and selective non-nucleoside PRMT5 inhibitor. The experimental process involved the reaction of 1-Methylpyrazole(cas: 930-36-9Application In Synthesis of 1-Methylpyrazole)
1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Application In Synthesis of 1-Methylpyrazole
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics