10261-02-6Relevant 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)
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.
Photooxidation of Some Triaza-and Tetraazabenzopentalenes
Albini, Angelo,Bettinetti, Gian Franco,Minoli, Giovanna
, p. 1080 - 1083 (1983)
The dye-sensitized photooxidation of some tri- and tetraazabenzopentalenes is reported.The pyrazolobenzotriazole 4 is converted to a mixture of 3-(1-benzotriazolyl)- and 3-(2-benzotriazolyl)propenals (7 and 8) in inert solvents, while in methanol the corr
3-AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 69, (2009/08/16)
The present invention relates to 3-azabicyclo[3.1.0]hexane derivatives, which are useful as vanilloid receptor (VR) ligands, methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
Chemistry of Tetraazapentalenes
Altmann, Karen L.,Chafin, Andrew P.,Merwin, Lawrence H.,Wilson, William S.,Gilardi, Richard
, p. 3352 - 3354 (2007/10/03)
2,4,8,10-Tetranitrobenzotriazolo[2,1-a]benzotriazole (TACOT), although thermally very stable and insensitive as an explosive, is susceptible to attack by nucleophiles. Reaction with azide ion results in displacement of nitro groups at the 4,10-positions, treatment with methoxide ion effects displacement of the hydrogen atom at the 1-position and scission of the remote triazole ring, while "vicarious nucleophilic animation" displaces all the aromatic hydrogens. 3,5,7-Trinitro-1,2,3-triazolo[2,1-a]benzotriazole and 3,5,7-trinitro-1,2,3-triazolo[1,2-a]benzotriazole are prepared readily by nitration of the parent triazolobenzotriazoles. However they are thermally less stable than TACOT and more sensitive to initiation by impact. Furthermore, attempted further nitration and reaction with nucleophiles such as azide and methoxide ions both effect scission of the triazole ring to leave 4,6-dinitrobenzotriazole.
