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Article

Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.

European journal of medicinal chemistry - 1 Jan 2018

Wang Yu, Chen Shaowei, Hu Gang, Wang Jiao, Gou Wenfeng, Zuo Daiying, Gu Yucheng, Gong Ping, Zhai Xin

Abstract excerpt

Aiming to explore novel anaplastic lymphoma kinase (ALK) and proto-oncogene tyrosine-protein kinase ROS (ROS1) dual inhibitors to overcome crizotinib-resistant mutants, two series of 2,4-diarylaminopyrimidine (DAAP) analogues bearing thiazole or 1,2,3-triazole moieties were designed and synthesized based upon the cocrystal structure of ceritinib with ALKWT (PDB 4MKC) as well as the binding model of ceritinib with...

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Source

Identifiers

PMID: 29174809
DOI: 10.1016/j.ejmech.2017.11.008

Genes

ALK
ROS1

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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