Design, synthesis, and anticancer assessment of structural analogues of ()-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2-]quinoxaline-2-carbonitrile (6b), an imidazo[1,2-]quinoxaline-based non-covalent EGFR inhibitor.

In our quest to find improved anticancer therapeutics, we expedite the lead optimization of ()-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2-]quinoxaline-2-carbonitrile (6b), an EGFR inhibitor previously discovered in our laboratory through an in-house screening program. The lead optimization was rationally initiated considering the catalytic site of EGFR. We synthesized twenty-nine new analogues of 6b and assessed their anticancer activities.