Article
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors.
Bioorganic & medicinal chemistry - 15 Jul 2022
Wang Xinyue, Hu Yiran, Zou Xinyu, Wang Pengfei, Yue Hao, Guo Mingzhang, Li Zefei, Gong Ping
Abstract excerpt
To overcome drug resistance caused by ALK kinase mutations especially G1202R, two series of novel 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety were designed, synthesized and evaluated for their biological activities. Among all the target compounds, B10 efficiently inhibited the proliferation of ALK-positive Karpas299 and H2228 cells both with IC50 values of 0.07 μM. In addition, B10...
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