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 new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation.

European journal of medicinal chemistry - 5 Sept 2024

Yao Han, Ren Yuanyuan, Wu Feng, Liu Jiadai, Li Jianheng, Cao Longcai, Yan Ming, Li Xingshu

Abstract excerpt

The C797S mutation of EGFR leads to Osimertinib resistance by blocking the covalent binding of Cys797. To develop new agents that can overcome EGFR mutation resistance, thirty seven new cyclopropane sulfonamide derivatives were synthesized and evaluated as EGFRL858R/T790M/C797S or EGFRDel19/T790M/C797S inhibitors by structure-based screening. Most of the synthesized compounds exhibit good to excellent anti...

Read the complete abstract on PubMed

Topics

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

Share to Cyclopropanes
Share to Drug Discovery

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Resistance, Neoplasm

Share to Drug Screening Assays, Antitumor

Share to Mice, Nude

Share to Molecular Structure

Share to Structure-Activity Relationship

Share to Sulfonamides

Source

Identifiers

PMID: 38908104
DOI: 10.1016/j.ejmech.2024.116590

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.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation.PMID 38908104Read ↗

Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance.Semantic proximity Read ↗

CZC54252 overcomes Osimertinib resistance by targeting EGFRC797S mutations.Semantic proximity Read ↗

Modification of osimertinib to discover new potent EGFRC797S-TK inhibitors.Semantic proximity Read ↗

Design, synthesis, and antitumor activity evaluation of potent fourth-generation EGFR inhibitors for treatment of Osimertinib resistant non-small cell lung cancer (NSCLC).Semantic proximity Read ↗

Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment.Semantic proximity Read ↗

Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.Semantic proximity Read ↗

Design, synthesis and biological evaluation of 2,4,5-trisubstituted 7H-Pyrrolo[2,3-d]pyrimidine derivatives as potent EGFR tyrosine kinase inhibitors against the C797S acquired resistance mutation.Semantic proximity Read ↗

Design and synthesis of 4th generation EGFR inhibitors against human triple (Del19/T790M/C797S) mutation.Semantic proximity Read ↗

Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Semantic proximity Read ↗

Design, Synthesis, and Biological Evaluation of Novel Diaminopyrimidine Macrocycles as Fourth Generation Reversible EGFR Inhibitors That Overcome Clinical Resistance to Osimertinib Mediated by C797S Mutation.Semantic proximity Read ↗

LS-106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo.Semantic proximity Read ↗

Repurposing CZC54252 to target EGFR C797S mutations and conquer Osimertinib resistanceSemantic proximity Read ↗

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