TL;DR
Combined computational and preliminary cell-based findings support compound 4i as a promising lead for further investigation of EGFR-targeted anticancer activity and biochemical EGFR kinase inhibition and target-engagement studies are required to determine the mechanism of action.
Two novel classes of hybrid quinazolin-2,4-diones 2–17, privileged with urea and/or carbamate moieties, as EGFR-TK inhibitors represent promising lead candidates for developing novel EGFR inhibitors for cancer treatment.
A number of lead candidates with strong EGFR inhibitory potential, promising pharmacokinetic profiles, and mutant selectivity were successfully identified by the integrated computational approach.
A novel series of benzofuran-based aryl urea derivatives incorporating a 1,3,4-thiadiazole linker were designed as dual VEGFR-2/BRAFWT inhibitors using sorafenib as a pharmacophoric template, with compound 7j emerging as the most active analogue.
This comprehensive review systematically examines recent advances in the rational design, synthesis, and biological evaluation of five-membered heterocyclic scaffolds, thiadiazol, oxazole, thiazole, thiazole, and pyrrole, as well as pyrazole and imidazole-based inhibitors as novel VEGFR-2 inhibitors.
Overall, the combined computational and biological findings suggest that amino quinoxaline scaffolds indicate potential avenues for enhanced optimization as EGFR-targeted anticancer drugs.
Findings highlight compound 5d as a promising lead candidate for further optimization and cellular mechanistic validation in anti-cancer drug discovery.
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