Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors was written by Li, Na;Yang, Hong;Liu, Ke;Zhou, Liwei;Huang, Yuting;Cao, Danyan;Li, Yanlian;Sun, Yaoliang;Yu, Aisong;Du, Zhiyan;Yu, Feng;Zhang, Ying;Wang, Bingyang;Geng, Meiyu;Li, Jian;Xiong, Bing;Xu, Shilin;Huang, Xun;Liu, Tongchao. And the article was included in Journal of Medicinal Chemistry in 2022.Safety of 4-Bromo-1-methylimidazole This article mentions the following:
A series of NSD2-PWWP1 inhibitors I (R = 4-cyanophenyl, 4-cyanonaphthalen-1-yl, 8-cyanoquinolin-5-yl, etc.; R1 = H, OMe, F, Cl, CF3; R2 = H, Me, OMe; R3 = aminomethyl, CHO, 4-aminopiperidin-1-yl, etc.), and further structure-based optimization resulted in a potent inhibitor compound I (R = 4-cyanonaphthalen-1-yl; R1 = R2 = Me; R3 = 4-aminopiperidin-1-yl) (II), that has high selectivity toward the NSD2-PWWP1 domain were reported. The detailed biol. evaluation revealed that compound II can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. The current discovery will provide a useful chem. probe to the future research in understanding the specific regulation mode of NSD2 by PWWP1 recognition and pave the way to develop potential drugs targeting NSD2 protein. In the experiment, the researchers used many compounds, for example, 4-Bromo-1-methylimidazole (cas: 25676-75-9Safety of 4-Bromo-1-methylimidazole).
4-Bromo-1-methylimidazole (cas: 25676-75-9) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.Safety of 4-Bromo-1-methylimidazole
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem