Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells was written by Cherian, Joseph;Nacro, Kassoum;Poh, Zhi Ying;Guo, Samantha;Jeyaraj, Duraiswamy A.;Wong, Yun Xuan;Ho, Melvyn;Yang, Hai Yan;Joy, Joma Kanikadu;Kwek, Zekui Perlyn;Liu, Boping;Wee, John Liang Kuan;Ong, Esther HQ;Choong, Meng Ling;Poulsen, Anders;Lee, May Ann;Pendharkar, Vishal;Ding, Li Jun;Manoharan, Vithya;Chew, Yun Shan;Sangthongpitag, Kanda;Lim, Sharon;Ong, S. Tiong;Hill, Jeffrey;Keller, Thomas H.. And the article was included in Journal of Medicinal Chemistry in 2016.Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:
Clin. used BCR-ABL1 inhibitors for the treatment of chronic myeloid leukemia do not eliminate leukemic stem cells (LSC). It has been shown that MNK1 and 2 inhibitors prevent phosphorylation of eIF4E and eliminate the self-renewal capacity of LSCs. Herein, the authors describe the identification of novel dual MNK1 and 2 and BCR-ABL1 inhibitors, starting from the known kinase inhibitor. Initial structure-activity relationship studies resulted in a compound with loss of BCR-ABL1 inhibition. Further modification led to orally bioavailable dual MNK1 and 2 and BCR-ABL1 inhibitors I and II, which are efficacious in a mouse xenograft model and also reduce the level of phosphorylated eukaryotic translation initiation factor 4E in the tumor tissues. Kinase selectivity of these compounds is also presented. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).
4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics