Design, synthesis and biological evaluation of a novel series of 1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety as cytotoxic agents

  • Eur J Med Chem. 2012 Jul:53:203-10. doi: 10.1016/j.ejmech.2012.03.056.
Pushpan Puthiyapurayil  1 ,  Boja Poojary ,  Chandrashekhar Chikkanna ,  Sunil Kumar Buridipad
Affiliations
  • 1. Department of Chemistry, Mangalore University, Mangalagangotri 574199, Karnataka, India. [email protected]
PMID: 22542958 DOI: 10.1016/j.ejmech.2012.03.056
Abstract

On account of the reported Anticancer activity of pyrazoles and oxadiazoles, we have designed and synthesized a novel combinatorial library of S-substituted-1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety and tested for in-vitro cytotoxic activity by MTT assay. Amongst the tested compounds, the compound 5e was the most promising Anticancer agent with IC(50) value of 15.54 μM in MCF-7 cells, compared to Doxorubicin as standard drug. The newly synthesized compounds were characterized by NOE, IR, (1)H NMR, (13)C NMR and LC-MS analysis.