A series of 2-chloro-N-(3-cyano-4,6-diphenylpyridin-2-yl)acetamide derivatives were synthesized using substituted aromatic amines. The chemistry of the reactions employed in the synthesis of the target compounds along with biological properties are discussed in the research work. The synthesized compounds were satisfactorily characterized by IR, 1H and 13C NMR spectrum. Five synthesized compounds (6a-6e) were tested for in vitro anticancer activity against MCF-7 cell line. The in vitro anticancer activity was based upon the MTT assay method. The anticancer activity results showed that, among the tested compounds, compound 6a, 6d and 6e were found to be most active with IC50 value 50 mig.