Novel 2-amino-4-(1H-imidazol)pyridine derivatives as potent brain-penetrant EGFR mutant inhibitors: Design, synthesis, biological evaluation, and molecular modeling study.

Abstract excerpt

EGFR inhibitors, including Osimertinib, have achieved marked success in treating non-small-cell lung cancer (NSCLC). However, major challenges persist, including clinical resistance mutations in NSCLC and limited efficacy against EGFR-altered glioblastoma (GBM). This underscores the urgent need for brain-penetrant EGFR inhibitors capable of circumventing mutant resistance and targeting EGFR-driven GBM. To address...

Topics

• Humans
• ErbB Receptors
• Protein Kinase Inhibitors
• Antineoplastic Agents
• Drug Design