A series of 2-arylbenzo[b]furan–appended 4-aminoquinazoline hybrids were prepared and evaluated for
cytotoxicity in vitro against the human lung cancer (A549), colorectal adenocarcinoma (Caco-2), hepatocellular
carcinoma (C3A) and cervical cancer (HeLa) cell lines. Compounds 10d and 10j exhibited significant
cytotoxicity against the C3A and Caco-2 cell lines and induced apoptosis in these cell lines. Likewise,
compounds 10d and 10e exhibited significant inhibitory activity towards epidermal growth factor receptor-
tyrosine kinase phosphorylation (IC50 values of 29.3 nM and 31.1 nM, respectively) against Gefitinib
(IC50¼33.1 nM). Molecular docking of compounds 10 into EGFR-TK active site suggests that they bind to
the region of EGFR like Gefitinib does.