Cui, Yi-Man; Li, Wei; Shen, Tian-Ze; Tao, Yong-Xing; Liu, Biao-Qi; Li, Xiao-Li; Zhang, Rui-Han; Jiang, De-Wei; Xiao, Wei-Lie published the artcile< Design, synthesis and anti-breast cancer evaluation of biaryl pyridine analogues as potent RSK inhibitors>, Category: piperazines, the main research area is antitumor biaryl pyridine breast cancer; biaryl pyridine preparation RSK kinase inhibitor mol docking; Breast Cancer; LJH685; RSK inhibitor; Structure-activity relationship; YB-1 phosphorylation.
In order to discover and develop new RSK kinase inhibitors, 50 pyridyl biaryl derivatives were designed and synthesized with LJH685 as the lead compound and their anti-tumor ability was tested. The results showed that the ability of compound 3-pyridine derivative I to inhibit the phosphorylation of YB-1 was comparable to that of LJH685. Among the synthesized compounds, after a preliminary screening, compound I showed good activity at inhibiting cell proliferation. Therefore, the authors took I as an example and performed mol. docking anal. on it. Judging from the overlapping combination diagram with LJH685, the results have verified that compound I has a similar skeleton to LJH685 and has a similar docking effect with RSK. Therefore, compound I is in line with the RSK inhibitor the authors designed and could be developed into a promising anti-tumor drug in the future.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Category: piperazines.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics