The author of 《Design, synthesis, and anticancer activity of imidazo[2,1-b]oxazole-based RAF kinase inhibitors》 were Abdel-Maksoud, Mohammed S.; Ammar, Usama M.; El-Gamal, Mohammed I.; Gamal El-Din, Mahmoud M.; Mersal, Karim I.; Ali, Eslam M. H.; Yoo, Kyung Ho; Lee, Kyung-Tae; Oh, Chang-Hyun. And the article was published in Bioorganic Chemistry in 2019. Application of 98-60-2 The author mentioned the following in the article:
A novel series of B-RAF kinase inhibitors having imidazo[2,1-b]oxazole scaffold I [R = H, F; n = 1, 2; Ar = 4-methylphenyl, naphthalen-1-yl, 4-(trifluoromethyl)phenyl, etc.] was designed and synthesized based on the structures of the well-known B-RAF inhibitors. The twenty two final compounds I were tested over A375 and SKMEL28 cell lines to determine the primary cytotoxic activity of these compounds and their activities were compared with that of sorafenib as a standard Compounds I [R = H, n = 1, Ar = 4-chlorophenyl; R = H, n = 2, Ar = 4-(trifluoromethyl)phenyl; R = F, n = 2, Ar = phenyl; R = F, n = 2, Ar = 4-methylphenyl; R = F, n = 2, Ar = 4-(trifluoromethyl)phenyl, R = F, n = 2, Ar = 4-fluorophenyl] exhibited higher cellular activity compared to sorafenib with IC50 values of 7.25, 8.03, 9.81, 8.47, 4.70 and 9.04 μM, resp. and 10.38 μM for sorafenib. In addition, the target compounds were screened for their anticancer activity by the NCI-60 cell line assay. Compounds I [R = F, n = 2, Ar = naphthalen-1-yl; R = F, n = 2, Ar = 4-fluorophenyl] were the most active compounds with percent inhibition reached 95.99% for I [R = F, n = 2, Ar = naphthalen-1-yl] and 87.03% for I [R = F, n = 2, Ar = 4-fluorophenyl] over K562 cell line at 10 μM concentration Compound I [R = F, n = 2, Ar = naphthalen-1-yl] was selected for 5-dose test mode. Furthermore, the kinase inhibitory activities of I [R = H, n = 1, Ar = 4-methylphenyl; R = H, n = 1, Ar = 4-chlorophenyl; R = H, n = 2, Ar = 4-(trifluoromethyl)phenyl; R = F, n = 1, Ar = 4-methylphenyl; R = F, n = 2, Ar = phenyl; R = F, n = 2, Ar = 4-methylphenyl; R = F, n = 2, Ar = 4-(trifluoromethyl)phenyl; R = F, n = 2, Ar = 4-fluorophenyl; R = F, n = 2, Ar = naphthalen-1-yl] were determined against wild-type B-RAF, V600E-B-RAF and RAF1. Compound I [R = F, n = 2, Ar = phenyl] was the most potent against V600E-B-RAF with IC50 34 nM followed by I [R = F, n = 2, Ar = 4-methylphenyl; R = F, n = 2, Ar = 4-fluorophenyl] with IC50 92 and 93 nM, resp. In addition to this study using 4-Chlorobenzenesulfonyl chloride, there are many other studies that have used 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Application of 98-60-2) 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.Application of 98-60-2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics