Name: 3-Chloro-4-fluoronitrobenzeneOn November 15, 2021 ,《The synthesis and bioactivity of pyrrolo[2,3-d]pyrimidine derivatives as tyrosine kinase inhibitors for NSCLC cells with EGFR mutations》 appeared in European Journal of Medicinal Chemistry. The author of the article were Xia, Zhenqiang; Huang, Ridong; Zhou, Xinglong; Chai, Yingying; Chen, Hai; Ma, Lingling; Yu, Quanwei; Li, Ying; Li, Weimin; He, Yang. The article conveys some information:
A series of pyrrolo[2,3-d]pyrimidine derivatives able to block mutant EGFR activity in a covalent manner were synthesized, through optimized Buchwald-Hartwig C-N cross coupling reactions. Their preliminary bioactivity and corresponding inhibitory mechanistic pathways were investigated at mol. and cellular levels. Several compounds exhibited increased biol. activity and enhanced selectivity compared to the control compound Notably, N-(3-((2-((3-amino-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-cyclopenta[d]pyrimidin-4-yl)oxy)phenyl)acrylamide selectively inhibits HCC827 cells harboring the EGFR activating mutation with up to 493-fold increased efficacy compared to in normal HBE cells. Augmented selectivity was also confirmed by kinase enzymic assay, with the test compound selectively inhibiting the T790 M activating mutant EGFRs (IC50 values of 0.21 nM) with up to 104-fold potency compared to the wild-type EGFR (IC50 values of 22 nM). Theor. simulations provided structural evidence of selective kinase inhibitory activity. Thus, this series of pyrrolo[2,3-d]pyrimidine derivatives could serve as a starting point for the development of new EGFR-TKIs. In the experiment, the researchers used 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Name: 3-Chloro-4-fluoronitrobenzene)
3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. Name: 3-Chloro-4-fluoronitrobenzene 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.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics