38154-38-0Relevant academic research and scientific papers
Discovery of novel 2,4-diarylaminopyrimidine derivatives as potent and selective epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M resistance mutation
Yan, Qi,Chen, Yuzhe,Tang, Baiyou,Xiao, Qiang,Qu, Rong,Tong, Linjiang,Liu, Jian,Ding, Jian,Chen, Yi,Ding, Ning,Tan, Wenfu,Xie, Hua,Li, Yingxia
, p. 298 - 306 (2018/05/22)
A series of novel 2,4-diarylaminopyrimidine derivatives of AZD9291 were discovered as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. The majority of these compounds exhibited moderate to excellent EGFR T790 M/L858R inhibitory activities and comparable anti-proliferative activities against double mutant over-expressed NCI-H1975 cells to that of AZD9291. The most promising compounds 8a displayed an IC50 of 4.1 nM against EGFR L858R/T790M mutants. 8a also showed excellent cytotoxic effect against NCI-H1975 cells with an IC50 of 59 nM and 100-fold selectivity over wide-type EGFR over-expressed A431 cells. Compound 8a significantly inhibited tumor growth in NCI-H1975 xenograft models at a non-toxic dose. Docking study performed for 8a with ATP binding site of EGFR-TK showed the similar binding mode to that of AZD9291. All these results suggested that compound 8a was a potential mutant-selective EGFR inhibitor.
Rearrangement in Heterocyclic Synthesis. 2. Novel Transformations of 2-Aminonicotinonitrile and Anthranilonitrile
Hosmane, Ramachandra S.,Lim, Benjamin B.,Summers, Michael F.,Siriwardane, Upali,Hosmane, Narayan S.,Chu, Shirley S. C.
, p. 5309 - 5315 (2007/10/02)
Methyl N-(3-cyanopyridin-2yl)methanimidate (4) was prepared by the reaction of 2-aminonicotinonitrile with trimethyl orthoformate, catalyzed by trifluoroacetic acid.Treatment of 4 with methylhydrazine at 0 deg C provided N-amino-N-methyl-N'-(3-cyanopyridi
