Abdel-Maksoud, Mohammed S.; Mohamed, Ahmed A. B.; Hassan, Rasha M.; Abdelgawad, Mohamed A.; Chilingaryan, Garri; Selim, Samy; Abdel-Bakky, Mohamed S.; Al-Sanea, Mohammad M. published their research in International Journal of Molecular Sciences in 2021. The article was titled 《Design, Synthesis and Anticancer Profile of New 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-Linked Sulfonamide Derivatives with V600EBRAF Inhibitory Effect》.Electric Literature of C6H4Cl2O2S The article contains the following contents:
A series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives, I [R = 4-fluorophenyl, 4-methoxyphenyl, 1-naphthyl, etc., n = 1, 2] was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series I was tested at fixed concentration (1μM) against V600EBRAF, finding that I [R = 4-fluorophenyl, n = 2; R = 4-trifluoromethyl, n = 1, 2] exhibited the strongest inhibitory activity among all target compounds and I [R = 4-trifluoromethyl, n = 2] had the lowest IC50 of 0.49μM. They were further screened on NCI 60 cancer cell lines to reveal that I [R = 4-trifluoromethyl, n = 1] showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle anal. of I [R = 4-trifluoromethyl, n = 1] was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, I [R = 4-fluorophenyl, n = 2; R = 4-trifluoromethyl, n = 1, 2]. In addition to this study using 4-Chlorobenzenesulfonyl chloride, there are many other studies that have used 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Electric Literature of C6H4Cl2O2S) was used in this study.
4-Chlorobenzenesulfonyl chloride(cas: 98-60-2) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Electric Literature of C6H4Cl2O2S
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics