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 published the artcile< Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors>, Category: imidazoles-derivatives, the main research area is imidazole preparation SAR antitumor activity inhibitor.
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.
Journal of Medicinal Chemistry published new progress about Amines Role: PAC (Pharmacological Activity), PKT (Pharmacokinetics), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Category: imidazoles-derivatives.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem