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Article

Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.

European journal of medicinal chemistry - 20 Jan 2018

Geng Kaijun, Xia Zongjun, Ji Yinchun, Zhang Ruisi Ruthy, Sun Deqiao, Ai Jing, Song Zilan, Geng Meiyu, Zhang Ao

Abstract excerpt

To address drug resistance caused by ALK kinase mutations, especially the most refractory and predominant mutation G1202R for the second-generation ALK inhibitor, a series of new diarylaminopyrimidine analogues were designed by incorporating a resorcinol moiety (A-ring) to interact the ALK kinase domain where the G1202R is located. Compound 12d turns out as the most potent with IC50 values of 1.7, 3.5, and 1.8 nM...

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Identifiers

PMID: 29288940
DOI: 10.1016/j.ejmech.2017.12.060

Genes

ALK

Variants

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