New phenylcyclopropane-carbohydrazide furan derivatives with potent anticancer activity and EGFR inhibitory potential
Abstract
Fifteen new phenylcyclopropane-carbohydrazide-containing furan derivatives are synthesised and thoroughly characterized using FT-IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy techniques in the search for new anticancer drugs. Using the MTT assay, this work examines the antiproliferative capability of these newly synthesized phenylcyclopropane hybrid compounds against cancer cell lines of the liver (HepG-2), lung (A549), and breast (MCF-7 and MDA-MB-231). Results indicated that with IC50 values of 2.08 ± 0.45, 2.15 ± 0.29, 2.17 ± 0.13, and 3.10 ± 0.32 µM for the MCF-7 cell line, compounds 8e, 8i, 8m, and 8n with p-dimethylamino, p-methoxy, p-hydroxy, and p-chloro-o-methoxy groups, respectively, showed the strongest antiproliferative activity, surpassing the reference drug doxorubicin in some cases. Among the synthesized compounds, 8e, 8j, 8m and 8n were the most active compounds with the EGFRWT inhibitory effect, exhibiting IC50 values of 1.79 ± 0.10, 1.59 ± 0.03, 0.87 ± 0.08, and 0.90 ± 0.60 µM, respectively. Molecular docking studies against the human breast cancer therapy compound and epidermal growth factor receptor (EGFR) (PDB codes: 3HB5 & 1M17) revealed that the furan derivatives exhibited excellent binding affinity (-10.70 and -8.54 kcal mol-1) through favorable van der Waals, electrostatic, HB-bonding and CH-bonding interactions within the active site. Furthermore, the ADME-T (absorption, distribution, metabolism, excretion, and toxicity) profiling of the synthesized…
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