A novel series of triazolylquinazolin-4-one derivatives have been synthesized and characterized by TLC, melting point, FT-IR, 1H NMR and mass spectroscopy data. The synthesized series of title compounds were subjected for docking studies using Schrodinger Glide software, evaluated for their potential to inhibit enzyme EGFR-tyrosine kinase followed by in-vitro anticancer activity by SRB assay method on HeLa, MCF-7, A-549 cell lines. The series of compounds shows anticancer activity probably by inhibiting the enzyme EGFR-tyrosine kinase.