《Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors》 was written by Han, Chun; Wan, Ledong; Ji, Hongbin; Ding, Ke; Huang, Zhangjian; Lai, Yisheng; Peng, Sixun; Zhang, Yihua. Quality Control of 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine And the article was included in European Journal of Medicinal Chemistry on April 22 ,2014. The article conveys some information:
Novel compounds were synthesized and biol. evaluated. Several ones exhibited stronger inhibitory activity than gefitinib against EGFR L858R/T790M and antiproliferative effects on H1975 and HCC827 cells. The 3-aminopropamide in some compoundslike compound I could be converted to the active acrylamide in the presence of arginine. Importantly, compound I showed improved stability relative to compound WZ4002 whose structure is same to I excepting an acrylamide moiety. Interestingly, compound II, a NO donating compound of I, showed more potent and selective inhibition than compound I on H1975 cells. Significantly, compound II produced high levels of NO in H1975 cells but not in non-tumorous 16HBE cells, and its inhibition was diminished by NO scavenger. Furthermore, compound II dose-dependently produced inhibitory effects on EGFR downstream signaling in H1975 cells. In the experiment, the researchers used 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine(cas: 1213269-26-1Quality Control of 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine)
4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine(cas: 1213269-26-1) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.Quality Control of 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics