Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway was written by 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. And the article was included in Bioorganic & Medicinal Chemistry in 2021.Quality Control of 2,4-Dichlorophenylisothiocyanate This article mentions 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. In the experiment, the researchers used many compounds, for example, 2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1Quality Control of 2,4-Dichlorophenylisothiocyanate).
2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Quality Control of 2,4-Dichlorophenylisothiocyanate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics