Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.

Bioorganic chemistry - 1 May 2022

An Baijiao, Liu Jian, Fan Yangyang, Nie Wenyan, Yang Chunhua, Yao Han, Li Wei, Zhang Yin, Li Xingshu, Tian Geng

Abstract excerpt

The critical T790M secondary mutation in epidermal growth-factor receptor (EGFR) mediates resistance to first- and second-generation EGFR tyrosine kinase inhibitors. Herein, we identified 12 new 2,4-diaryl pyrimidine derivatives containing thiophene fragments as new selective third-generation EGFR inhibitors. Among them, Compound 6a showed good inhibitory activity against EGFR mutant cells with an IC50 value of...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Antineoplastic Agents
Share to Carcinoma, Non-Small-Cell Lung

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cell Proliferation

Share to Drug Resistance, Neoplasm

Share to ErbB Receptors

Share to Protein Kinase Inhibitors

Share to Pyrimidines

Share to Structure-Activity Relationship

Source

Identifiers

PMID: 35313239
DOI: 10.1016/j.bioorg.2022.105743

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.PMID 35313239Read ↗

Novel EGFR inhibitors against resistant L858R/T790M/C797S mutant for intervention of non-small cell lung cancer.Semantic proximity Read ↗

The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.Semantic proximity Read ↗

Pan-EGFR inhibitor targeting EGFR 19del, L858R/T790M and C797S triple-mutations: Design, synthesis, and pharmacological evaluation.Semantic proximity Read ↗

Design, synthesis, and biological evaluation of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines as potent EGFRT790M/L858R inhibitors to treat non-small cell lung cancer.Semantic proximity Read ↗

Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.Semantic proximity Read ↗

Pyrimidine derivatives as EGFR tyrosine kinase inhibitors in non-small-cell lung cancer: A comprehensive review.Semantic proximity Read ↗

Design, synthesis and biological evaluation of potent epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors against resistance mutation for lung cancer treatment.Semantic proximity Read ↗

The advance of the third‑generation EGFR‑TKI in the treatment of non‑small cell lung cancer (Review).Semantic proximity Read ↗

Novel bioactive 2-phenyl-4-aminopyrimidine derivatives as EGFRDel19/T790M/C797S inhibitors for the treatment of non-small cell lung cancer.Semantic proximity Read ↗

Design, synthesis and evaluation of new pyrimidine derivatives as EGFRC797S tyrosine kinase inhibitors.Semantic proximity Read ↗

Insights into fourth generation selective inhibitors of (C797S) EGFR mutation combating non-small cell lung cancer resistance: a critical reviewSemantic proximity Read ↗

Structure-guided discovery of a potent 2-aryl-4-aminoquinazoline-based inhibitor overcoming osimertinib resistance driven by EGFR C797S mutation in NSCLC.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.