ReviewPharmaceuticals (Basel, Switzerland)2023
Structure-Activity Relationship Studies Based on Quinazoline Derivatives as EGFR Kinase Inhibitors (2017-Present).
Review in Pharmaceuticals (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed, 50 citations in OpenAlex.
- Quinazolinone-diarylpyrazole hybrids as dual EGFR/COX-2 inhibitors: antiproliferative, mechanistic, andRSC advances · 2026Article
- Synthesis of Quinazoline Derivatives and Mechanistic Approaches in Lung and Breast Cancers.Molecules (Basel, Switzerland) · 2026Article
- Design and Synthesis of Novel Morpholine-Derived Nitrogen-Rich Scaffolds as Multifunctional Anticancer and Antibacterial Agents: Biological Evaluation and Computational Studies.Pharmaceutics · 2026Article
- Drugs inducing interstitial lung disease: in silico analysis of their structures and targets.Molecular medicine (Cambridge, Mass.) · 2026Article
- The resistance landscape of EGFR tyrosine kinase inhibitors in advanced non-small cell lung cancer: molecular mechanisms and novel therapeutic strategies.Translational lung cancer research · 2026Review
- Dacomitinib as a First-Line Therapy for Advanced EGFR-Mutated Non-Small Cell Lung Cancer Without Brain Metastases: A Multicenter Retrospective Observational Study.Cancer medicine · 2026Observational
- Natural products as kinase inhibitors in lung cancer: molecular mechanisms, therapeutic potential, and clinical trials.Frontiers in pharmacology · 2026Review
- Clinical characteristics and outcomes of advanced EGFR-mutated NSCLC treated with 45 or 30 mg starting doses of dacomitinib: a retrospective multicenter analysis.Therapeutic advances in medical oncology · 2026Article
- Thiourea Derivatives for the Potential Treatment of Lung Cancer via the Inhibition of EGFR and Efflux Pumps: Synthesis,Anti-cancer agents in medicinal chemistry · 2026Article
- A Review on Anticancer Potential and Structure-Activity Relationships (SAR) of Novel EGFR/HER2 Inhibitors.Current topics in medicinal chemistry · 2026Review
- A case study of the application of AI to early stage drug discovery.Scientific reports · 2025Article
- Design, Synthesis, and Biological Evaluation ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Fourth-generation EGFR-TKI to overcome C797S mutation: past, present, and future.Journal of enzyme inhibition and medicinal chemistry · 2025Review
- DeepEGFR a graph neural network for bioactivity classification of EGFR inhibitors.Scientific reports · 2025Article
- Current progress of 1,2,3-triazole hybrids as EGFR inhibitors for cancer therapy - a literature review.RSC advances · 2025Review
- The current landscape of quinazoline derivatives withFuture medicinal chemistry · 2025Review
- The current landscape of quinazoline derivatives withFuture medicinal chemistry · 2025Review
- Synthesis of 4-tosyl quinazoline derivatives with the assistance of ultrasound irradiation as a guide to the reaction pathway.Scientific reports · 2025Article
- Recent advances in the investigation of the quinazoline nucleus and derivatives with potential anticancer activities.Future medicinal chemistry · 2025Review
- Optimizing Osimertinib for NSCLC: Targeting Resistance and Exploring Combination Therapeutics.Cancers · 2025Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of various forms of cancer. Targeting the mutant forms of EGFR has been identified as an attractive therapeutic approach and led to the approval of three generations of inhibitors. The quinazoline core has emerged as a favorable scaffold for the development of novel EGFR inhibitors due to increased affinity for the active site of EGFR kinase. Currently, there are five first-generation (gefitinib, erlotinib, lapatinib, vandetanib, and icotinib) and two second-generation (afatinib and dacomitinib) quinazoline-based EGFR inhibitors approved for the treatment of various types of cancers. The aim of this review is to outline the structural modulations favorable for the inhibitory activity toward both common mutant (del19 and L858R) and resistance-conferring mutant (T790M and C797S) EGFR forms, and provide an overview of the newly synthesized quinazoline derivatives as potentially competitive, covalent or allosteric inhibitors of EGFR.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.