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.
Keywords: 4-anilinoquinazoline, Anti-tumor activity, Epidermal growth factor receptor (EGFR).
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