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September 10, 2025Journal of Medicinal Chemistry

Discovery of Potent and Selective Pyrrolo2,3-dpyrimidine Derivatives as Fourth-Generation EGFR Inhibitors Targeting Triple Mutations

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Authors

ZWZhenhua WuXLXueyan LiuXYXiao-E Yan

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Overview

Identifying potent EGFR inhibitors to target triple mutations in nonsmall cell lung cancer, suggesting new treatments.

Key Points

  • Compound 31r demonstrates subnanomolar IC50 values against specific EGFR triple mutations, indicating high efficacy.
  • Inhibition of tumor growth in xenograft models highlights its potential as a therapeutic agent for drug-resistant NSCLC.
  • Cocrystal structure analysis provides insights into the binding mode and selectivity for mutant EGFR forms, improving understanding of treatment mechanisms.
  • Pyrrolo[2,3-d]pyrimidine derivatives exhibit good metabolic stability and oral bioavailability, supporting their development as drug candidates.

Cite This Study

Wu et al. (2025) studied this question.

synapsesocial.com/papers/68d413f8713b0b5dfea61b2ehttps://doi.org/10.1021/acs.jmedchem.5c01320
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Also Consider

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  1. 1Triazole‐Pyrimidine Hybrids as EGFR Inhibitors via Synthesis, In Silico, In Vitro, and In Vivo Evaluation as Anticancer Agents2025
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  3. 3Design and synthesis of novel 3,5-diphenyl pyrazolines acting as potent EGFR inhibitors with off-target antileukemic effect.2025
  4. 4Structure-Based Molecular Docking and ADME Profiling of Novel Thienopyrimidines as Dual VEGFR/EGFR Inhibitors in Colorectal Cancer2025
  5. 5Fragment-Based <i>De Novo</i> Discovery of Fourth-Generation EGFR-L858R/T790M/C797S-Tyrosine Kinase Inhibitors Targeting Catalytic Lys745 Residue to Overcome the Osimertinib Resistance2025