Discover Community Create You

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

Discovery of novel selective inhibitors for EGFR-T790M/L858R.

Bioorganic & medicinal chemistry letters - 1 Feb 2012

Bai Fang, Liu Hongyan, Tong Linjiang, Zhou Wei, Liu Li, Zhao Zhenjiang, Liu Xiaofeng, Jiang Hualiang, Wang Xicheng, Xie Hua, Li Honglin

Abstract excerpt

Through a receptor-based and ligand-based combined virtual screening protocol, 21 novel compounds covering 15 scaffolds were identified as novel inhibitors for EGFR-T790M/L858R, among which, 12 of them were identified as selective inhibitors for EGFR-T790M/L858R to wild-type EGFR, and 5 of them exhibited 'dual-effective' to wild-type and mutant EGFR. Meanwhile, their antiproliferative effects toward EGFR...

Read the complete abstract on PubMed

Topics

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

Share to Catalytic Domain
Share to Cell Line, Tumor

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cell Proliferation

Share to Drug Discovery

Share to ErbB Receptors

Share to Inhibitory Concentration 50

Share to Molecular Structure

Share to Protein Kinase Inhibitors

Source

Identifiers

PMID: 22227214
DOI: 10.1016/j.bmcl.2011.12.067

Genes

EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of novel selective inhibitors for EGFR-T790M/L858R.PMID 22227214Read ↗

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

Chemical Scaffolds for the Clinical Development of Mutant-Selective and Reversible Fourth-Generation EGFR-TKIs in NSCLC.Semantic proximity Read ↗

Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants.Semantic proximity Read ↗

A high-throughput cell-based screening for L858R/T790M mutant epidermal growth factor receptor inhibitors.Semantic proximity Read ↗

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

Design, synthesis and biological evaluation of EGFR kinase inhibitors that spans the orthosteric and allosteric sites.Semantic proximity Read ↗

Novel anilinopyrimidine derivatives as potential EGFRT790M/C797S Inhibitors: Design, Synthesis, biological activity study.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 potent epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors against resistance mutation for lung cancer treatment.Semantic proximity Read ↗

Epidermal growth factor receptor dual-target inhibitors as a novel therapy for cancer: A review.Semantic proximity Read ↗

Epidermal growth factor receptors unveiled: a comprehensive survey on mutations, clinical insights of global inhibitors, and emergence of heterocyclic derivatives as EGFR inhibitors.Semantic proximity Read ↗

Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant.Semantic proximity Read ↗

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