Design, synthesis, and biological evaluation of novel quinoline-based EGFR/HER-2 dual-target inhibitors as potential anti-tumor agents
Lamya H. Al-Wahaibi, Essmat M. El‐Sheref, Hendawy N. Tawfeek, Hesham A. Abou‐Zied, Safwat M. Rabea, Stefan Bräse, Bahaa G. M. Youssif
Abstract
= 26 nM) as a HER2 inhibitor. The apoptotic potential activity of 5a was examined, and the findings demonstrated that 5a promotes apoptosis by activating caspase-3, 8, and Bax while simultaneously reducing the expression of the anti-apoptotic protein Bcl-2. The docking studies provided valuable insights into the binding interactions of compounds 3e and 5a with EGFR, effectively rationalizing the observed SAR trends.
Topics & Concepts
QuinolineChemistryCombinatorial chemistryEGFR inhibitorsEpidermal growth factor receptorOrganic chemistryBiochemistryReceptorHER2/EGFR in Cancer ResearchCancer therapeutics and mechanismsLung Cancer Treatments and Mutations