4-Anilinoquinazoline Derivatives with Epidermal Growth Factor Receptor Inhibitor Activity

4-Anilinoquinazoline derivatives possess high anti-cancer activities. Many of them are highly selective tyrosine kinase inhibitors (TKI), particularly against epidermal growth factor receptor (EGFR). EGFRs are overexpressed or mutated in most carcinomas and are required for tumor progression. The efficacy of EGFR-targeted anti-tumor drugs is impaired by drug-induced acquired resistance. Therefore, there is urgency to find better anti-cancer agents with novel effects on EGFR. 4-Anilinoquinazolines are small molecule EGFR inhibitors that have been synthesized and assessed for their anti-tumor bioactivity. In this paper, we review the 4-anilinoquinazoline derivatives with EGFR inhibitor activity reported in recent years.