A variety of novel 1,2-dihydropyridines 10-17, thiophenes 18-21 and thiazole 22 having a biologically active sulfone moiety were obtained via the reaction of 2-cyano-N'-[1-(4-(piperidin-1-ylsulfonyl) phenyl) ethylidene] acetohydrazide 3 with a variety of reagents. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human breast cancer cell line (MCF7). Compounds 15 and 11 with IC(50) values (20.6, 25.5 μM) exhibited better activity than Doxorubicin as a reference drug with IC(50) value (32.02 μM), while compound 14 is nearly as active as Doxorubicin as positive control.