New cyanobenzofurans derivatives 2-12 were synthesised, and their antiproliferative activity was examined compared to doxorubicin and Afatinib (IC 50 ¼ 4.17-8.87 and 5.5-11.2 mM, respectively). Compounds 2 and 8 exhibited broad-spectrum activity against HePG2 (IC 50 ¼ 16.08-23.67 mM), HCT-116 (IC 50 ¼ 8.81-13.85 mM), and MCF-7 (IC 50 ¼ 8.36-17.28 mM) cell lines. Compounds 2, 3, 8, 10, and 11 were tested as EGFR-TK inhibitors to demonstrate their possible anti-tumour mechanism compared to gefitinib (IC 50 5 0.90 mM). Compounds 2, 3, 10, and 11 displayed significant EGFR TK inhibitory activity with IC 50 of 0.81-1.12 mM. Compounds 3 and 11 induced apoptosis at the Pre-G phase and cell cycle arrest at the G2/ M phase. They also increased the level of caspase-3 by 5.7-and 7.3-fold, respectively. The molecular docking analysis of compounds 2, 3, 10, and 11 indicated that they could bind to the active site of EGFR TK.
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