On August 1, 2021, Wang, Zhengjie; Liu, Limin; Dai, Honglin; Si, Xiaojie; Zhang, Luye; Li, Erdong; Yang, Zhang; Chao, Gao; Zheng, Jiaxin; Ke, Yu; Shan, Lihong; Zhang, Qiurong; Liu, Hongmin published an article.Related Products of 16230-24-3 The title of the article was Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway. And the article contained the following:
In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound I had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound I also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound I exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound I could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound I targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Mol. docking showed that compound I could bind into the active pocket of EGFR. Those work suggested that compound I would have remarkable implications for further design of anti-tumor agents. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Related Products of 16230-24-3
The Article related to quinazoline preparation antiproliferation antitumor mol docking apoptosis egfr, antiproliferation, cell cycle analysis, egfr, quinazoline, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 16230-24-3
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Amide – an overview | ScienceDirect Topics