Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction was written by Nan, Xiang;Zhang, Jing;Li, Hui-Jing;Wu, Rui;Fang, Sen-Biao;Zhang, Zhi-Zhou;Wu, Yan-Chao. And the article was included in European Journal of Medicinal Chemistry in 2020.Computed Properties of C8H9Cl This article mentions the following:
A series of new N-sulfonylamidine derivatives were designed, synthesized via Cu-catalyzed multicomponent reaction (MCR) as the key step, and evaluated for their in vitro biol. activities against c-Met kinase and four cancer cell lines (A549, HT-29, MKN-45 and MDA-MB-231). Most of the target compounds showed moderate to significant potency at enzyme and cell-based assay. The preliminary SAR studies demonstrated that compound I (c-Met IC50 = 2.89 nM) was the most promising compound compared with the pos. foretinib, which exhibited the remarkable antiproliferative activities, with IC50 values ranging from 0.28 to 0.72渭M. Mechanistic studies of compound I showed the anticancer activity was closely related to the blocking phosphorylation of c-Met, leading to cell cycle arresting at G2/M phase and apoptosis of A549 cells by a concentration-dependent manner. The promising compound I was further identified as a relatively selective inhibitor of c-Met kinase, which also possessed an acceptable safety profile and favorable pharmacokinetic properties in BALB/c mouse. The favorable drug-likeness of I suggested that N-sulfonylamidines may be used as a promising scaffold for antitumor drug development. Addnl., the docking study and mol. dynamics simulations of I revealed a common mode of interaction with the binding site of c-Met. These pos. results indicated that I is a potential anti-cancer candidate for clin. trials, and deserves further development as a selective c-Met inhibitor. In the experiment, the researchers used many compounds, for example, 1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9Computed Properties of C8H9Cl).
1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Computed Properties of C8H9Cl
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics