Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity
Amr Sonousi, Rasha A. Hassan, Eman O. Osman, Amr M. Abdou, Soha H. Emam
Abstract
showed 16.74-fold increase in total apoptosis and caused cell cycle arrest at G1/S phase in breast cancer HS 578T cell line. Moreover, the most potent derivatives were docked into the EGFR active site to determine their binding mode and confirm their ability to satisfy the pharmacophoric features required for EGFR inhibition.
Topics & Concepts
QuinazolinoneChemistryErlotinibApoptosisCell cycle checkpointIC50Cell cultureEGFR inhibitorsCell cycleIn vitroCell growthLead compoundPharmacologyStereochemistryCancer researchEpidermal growth factor receptorBiochemistryBiologyReceptorGeneticsQuinazolinone synthesis and applicationsCancer therapeutics and mechanismsSynthesis and biological activity