Synthesis and Evaluation of Some Novel 6-Substituted Quinazoline Derivatives as Antitumor Agents

Autor: Hai guan Ding Hai guan Ding, Zhi qiang Cai Zhi qiang Cai, Ling Hou Ling Hou, Zhi quan Hu Zhi quan Hu, Zheng sheng Jin Zheng sheng Jin, Di Xu Di Xu, Hui Cao Miao miao Meng Hui Cao Miao miao Meng, Yu Hui Xie Yu Hui Xie, De qiang Zheng De qiang Zheng
Rok vydání: 2019
Předmět:
Zdroj: Journal of the chemical society of pakistan. 41:186-186
ISSN: 0253-5106
Popis: 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.
Databáze: OpenAIRE
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