Design, synthesis, biological evaluation, and molecular docking of novel quinazolinone EGFR inhibitors as targeted anticancer agents

Abstract

The epidermal growth factor receptor (EGFR; ErbB-1; HER1) is the cellsurface receptor for members of the epidermal growth factor family. Overexpression and/or hyperactivation of EGFR kinase is associated with several human cancers such as lung, glioblastoma, and epithelian tumors of the neck and head, leading to the development of anticancer therapeutics targeting EGFR. The EGFR Kinase Assay Kit is designed to measure EGFR Kinase activity for screening and profiling applications using Kinase-Glo ® MAX as a detection reagent. The EGFR Kinase Assay Kit comes in a convenient 96-well format, with enough purified recombinant EGFR enzyme, EGFR substrate, ATP and Kinase Buffer 1 for 100 enzyme reactions.

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

“…Compound 52 a showed the most promising inhibitory potential for EGFR, with an IC 50 of 18.29 nM. [123] The hybridization of quinazoline and 7,8-dihydropyrido[4,3d]cpyrimidine scaffolds were conducted by Zhang and colleagues to target EGFR receptor. The conjugates were appraised against A431, A549 and H1975 cell lines, which demonstrated adequate antitumour activity.…”

“…Cycle arrest at the pre‐G1 and G2/M stages were defined by compound 52 a . Compound 52 a showed the most promising inhibitory potential for EGFR, with an IC 50 of 18.29 nM [123] …”