Abstract
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, 1H NMR, 13C 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 IC50 values (20.6, 25.5 μM) exhibited better activity than Doxorubicin as a reference drug with IC50 value (32.02 μM), while compound 14 is nearly as active as Doxorubicin as positive control.
A variety of novel 1,2-dihydropyridines 10–17, thiophenes 18–21 and thiazole 22 having a biologically active sulfone moiety were synthesized to evaluate their anti-breast cancer activity. Compounds 15 and 11 with IC50 values (20.6, 25.5 μM) exhibited better activity than Doxorubicin as a reference drug with IC50 value (32.02 μM), while compound 14 is nearly as active as Doxorubicin as positive control.▪
►Novel 1,2-dihydropyridine, thiophene and thiazole derivatives with significant anti-breast cancer activity. ►For 1,2-dihydropyridine derivatives, the most potent having p-chlorophenyl 15 and p-hydroxyphenyl 11. ►Also 1,2-dihydropyridine derivative 14 carrying p-Dimethylaminophenyl is nearly as active as the reference drug Doxorubicin as positive control.