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

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.

Journal of medicinal chemistry - 23 Mar 2017

Tomassi Stefano, Lategahn Jonas, Engel Julian, Keul Marina, Tumbrink Hannah L, Ketzer Julia, Mühlenberg Thomas, Baumann Matthias, Schultz-Fademrecht Carsten, Bauer Sebastian, Rauh Daniel

Abstract excerpt

The specific targeting of oncogenic mutant epidermal growth factor receptor (EGFR) is a breakthrough in targeted cancer therapy and marks a drastic change in the treatment of non-small cell lung cancer (NSCLC). The recurrent emergence of resistance to these targeted drugs requires the development of novel chemical entities that efficiently inhibit drug-resistant EGFR. Herein, we report the optimization process...

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 Drug Resistance, Neoplasm

Share to ErbB Receptors

Share to Indazoles

Share to Molecular Docking Simulation

Share to Protein Kinase Inhibitors

Source

Identifiers

PMID: 28225269
DOI: 10.1021/acs.jmedchem.6b01626

Genes

EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

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

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.PMID 28225269Read ↗

Noncovalent wild-type-sparing inhibitors of EGFR T790M.Semantic proximity Read ↗

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.Semantic proximity Read ↗

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.Semantic proximity Read ↗

Discovery of selective irreversible inhibitors for EGFR-T790M.Semantic proximity Read ↗

Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.Semantic proximity Read ↗

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.Semantic proximity Read ↗

Covalent EGFR Inhibitors: Binding Mechanisms, Synthetic Approaches, and Clinical Profiles.Semantic proximity Read ↗

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

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.Semantic proximity Read ↗

Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.Semantic proximity Read ↗

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.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.