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Article

Identification of highly potent 2,4-diarylaminopyrimidine analogs of a typical piperidinyl-4-ol moiety as promising antitumor ALK inhibitors.

Archiv der Pharmazie - 1 Dec 2023

Liu Shuyu, Wang Fuyi, Yang Juanjuan, Su Guangyue, Cao Zhi, Shan Mengya, Zhai Xin

Abstract excerpt

In light of the cocrystal structure of ceritinib with anaplastic lymphoma kinase (ALK)WT protein, a series of novel 2,4-diarylaminopyrimidine analogs (L1-L25) bearing a typical piperidinyl-4-ol moiety were designed and synthesized with improved biological and physicochemical properties. Satisfyingly, most compounds demonstrated moderate to excellent antitumor effects with IC50 values below 5 μM on ALK-positive...

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PMID: 37737557
DOI: 10.1002/ardp.202300416

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