184475-74-9Relevant academic research and scientific papers
Synthesis of several new quinazolin-4-amines containing p-toluenesulfonate moiety
Cai, Zhi-Qiang,Jin, Zheng-Sheng,Zheng, De-Qiang,Hou, Ling,Huang, Guan-Wang,Tian, Jun-Qiang,Wang, Guo-Jiang
, p. 573 - 575 (2016)
A series of novel quinazolin-4-amine derivatives containing p-toluenesulfonate moiety have been synthesised through the reaction of 4-chloro-7-methoxyquinazolin-6-yl acetate with substituted anilines in toluene solution at 90°C. Further treatment of the synthesised compound with ammonium hydroxide gave the corresponding substituted quinazoline derivatives which were subsequently processed through the sulfonyl reaction into quinazolin-4-amines containing p-toluenesulfonate moiety in DMF. Their structures were established by elemental analysis, IR and 1H NMR spectra.
Synthesis and evaluation of some novel 6-substituted quinazoline derivatives as antitumor agents
Ding, Hai-guan,Cai, Zhi-qiang,Hou, Ling,Hu, Zhi-quan,Jin, Zheng-sheng,Xu, Di,Cao, Hui,Meng, Miao-miao,Xie, Yu-Hui,Zheng, De-qiang
, p. 186 - 190 (2019/05/01)
Summry: A series of novel 6-substituted quinazoline derivatives were synthesised as epidermal growth factor receptor(EGFR) and Human epidermal growth factor receptor 2 (HER2)inhibitors in our lab. The novel compounds were measured for their dual enzyme inhibition as well as their cytotoxic activity on MCF7 cell line. The results revealed that all the compounds showed inhibition of both enzymes. Compound 5c showed the best inhibitory activity against both enzymes and IC50 of its was 2.6 nM against EGFR kinases and 4.3 nM against HER2 kinases, respectively. Most of the measured compounds showed to antitumor activity on MCF7.
Quinazoline derivatives
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, (2008/06/13)
The invention concerns quinazoline derivatives of the formula I STR1 wherein n is 1, 2 or 3 and each R2 is independently halogeno, trifluoromethyl or (1-4C)alkyl; R3 is (1-4C)alkoxy; and R1 is di-?(1-4C)alkyl!amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-?(1-4C)alkoxy-(2-4C)alkyl!amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R1 substituents comprising a CH2 (methylene) group which is not attached to a N or O atom optionally bears on said CH2 group a hydroxy substituent; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
