《Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants》 was published in Bioorganic & Medicinal Chemistry in 2020. These research results belong to Zhu, Minglin; Li, Wei; Zhao, Tianming; Chen, Yuxiang; Li, Tong; Wei, Shangfei; Guo, Ming; Zhai, Xin. Related Products of 109-01-3 The article mentions the following:
The ALK and ROS1 dual inhibitors had capable of overcoming crizotinib-resistant mutants, two series of 2,4-diarylaminopyrimidine derivatives were designed, synthesized and evaluated for their in-vitro cytotoxic activity. The 2,4-diarylaminopyrimidine scaffold and derivatize the DAAP scaffold with sulfonyl and acrylamide moieties to extend the structure-activity relationship (SAR) study was retained. Some compounds exhibited excellent inhibitory activity with a double-digit nanomolar level in MTT assay. Four compounds were selected for enzymic assays further, the results led to the identification of a potent ALK and ROS1 dual inhibitor I [R = 4-ethylpiperazinyl], with IC50 values of 3.7 nM, 2.3 nM, 8.9 nM and 1.9 nM against ALK, ALKL1196M, ALKG1202R and ROS1, resp. Ultimately, the mol. docking studies on I [R = 4-ethylpiperazinyl] clearly disclosed reasonable and optimal binding interactions with ALK. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3Related Products of 109-01-3)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Related Products of 109-01-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics