Many literature reports revealed the anticancer activity of
pyridine and
thiazole derivatives, especially in
lung cancer. Therefore, a new series of thiazolyl
pyridines linked with
thiophene moiety via
hydrazone group was prepared by one-pot multi-component reaction of (E)-1-(4-methyl-2-(2-(1-(thiophen-2-yl)ethylidene)hydrazinyl)thiazol-5-yl)ethanone with
benzaldehyde derivatives and
malononitrile in a good yield. Then, compound 5 and the thiazolyl
pyridines were investigated for their in vitro anticancer activity against
lung cancer (A549) cell line using MTT assay compared to
doxorubicin as a reference drug. The structure of all the newly synthesized compounds was established based on spectroscopic data and elemental analyses. For better insight to investigate their mechanism of action on A549 cell line, docking studies were performed, targeting
epidermal growth factor receptor (EGFR)
tyrosine kinase. The results obtained revealed that the tested compounds displayed excellent anticancer activities against
lung cancer cell line except 8c and 8f compared to reference drug. Based on the data obtained, it can be inferred that the novel compounds, as well as their key intermediate, compound 5, demonstrated potent anticancer activity against lung
carcinoma by inhibiting EGFR.