In this study, a new compound namely 1-((2-hydroxynaphthalen-1-yl)methyleneamino)-5-(4-methybenzoyl)-4-p-tolylpyrimidin-2(1H)-one (S2) was synthesized as a Schiff base using 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (S1) with 2-hydroxy-1-naphthaldehyde in 80% yield. Then, eight novel metal complexes (S3-S10) including Ni(II), Cu(II), Co(II), Ag(I), Pd(II), Pt(II), Cr(III), and Mn(II) metal ions were prepared from this new Schiff base (S2). The characterization of these complexes was done using H-1 NMR, C-13 NMR, LC-MS, IR, magnetic susceptibility and conductivity measurements. The anticancer activities of compounds (S3-S10) were tested against human epithelial lung carcinoma cell line (A549) for 72 h. All complexes demonstrated antiproliferative activity in A549 cell line and low half-maximal inhibitory concentration (IC50) values were calculated with GraphPad Prism program.