Anti-breast cancer activity of some novel 1,2-dihydropyridine, thiophene and thiazole derivatives

Eur J Med Chem. 2011 Jan;46(1):137-41. doi: 10.1016/j.ejmech.2010.10.024. Epub 2010 Oct 29.

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, (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.

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / pathology*
  • Cell Line, Tumor
  • Dihydropyridines / chemistry
  • Dihydropyridines / pharmacology
  • Dihydropyridines / therapeutic use
  • Humans
  • Inhibitory Concentration 50
  • Structure-Activity Relationship
  • Thiazoles / chemistry
  • Thiazoles / pharmacology
  • Thiazoles / therapeutic use
  • Thiophenes / chemistry
  • Thiophenes / pharmacology
  • Thiophenes / therapeutic use

Substances

  • Antineoplastic Agents
  • Dihydropyridines
  • Thiazoles
  • Thiophenes
  • 1,4-dihydropyridine