Synthesis, characterization and anticancer screening of some novel piperonyl-tetrazole derivatives

Eur J Med Chem. 2014 Jan:71:229-36. doi: 10.1016/j.ejmech.2013.11.008. Epub 2013 Nov 15.

Abstract

A series of new 1,2-substituted tetrazole derivatives were synthesized and evaluated on MCF-7 (ER positive), MDA-MB-231 and ZR-75 (ER negative) breast cancer cell lines. Out of the fourteen compounds, three compounds 10, 12 and 14 showed higher inhibitory effects on MCF-7 cells. Whereas, compound 8 exhibited higher inhibition in MDA-MB-231 and ZR-75 cells at 10(-5) M concentration. Total RNA was extracted and effect of compounds on different marker genes was studied. The gene expression of CD44, BRAC and BAX were significantly affected. The compounds were screened against the HepG2 cell line, to know if they are selectively targeting specific cancers and only 1-10 percent inhibition was found at 10(-5) M concentration.

Keywords: Anticancer; MCF-7; MDA-MB-231; Tetrazole derivatives; ZR-75.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Breast / drug effects
  • Breast / metabolism
  • Breast / pathology
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Female
  • Humans
  • MCF-7 Cells
  • RNA / genetics
  • RNA / isolation & purification
  • Tetrazoles / chemical synthesis
  • Tetrazoles / chemistry*
  • Tetrazoles / pharmacology*

Substances

  • Antineoplastic Agents
  • Tetrazoles
  • 1H-tetrazole
  • RNA