期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 1, 页码 137-141出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.10.024
关键词
Sulfones; 1,2-Dihydropyridines; Thiophenes; Thiazole; Anticancer activity
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, H-1 NMR, C-13 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 mu M) exhibited better activity than Doxorubicin as a reference drug with IC50 value (32.02 mu M), while compound 14 is nearly as active as Doxorubicin as positive control. (C) 2010 Elsevier Masson SAS. All rights reserved.
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