New Chiral Ebselen Analogues with Antioxidant and Cytotoxic Potential

Molecules. 2017 Mar 20;22(3):492. doi: 10.3390/molecules22030492.

Abstract

New chiral camphane-derived benzisoselenazol-3(2H)-ones and corresponding diselenides have been synthetized using a convenient one-pot procedure. Se-N bond was efficiently converted to an Se-Se bond, which could also be easily re-oxidized to the initial benzisoselenazolone moiety. The antioxidant activity of camphor derivatives was evaluated and compared to the reactivity of a series of N-amino acid benzisoselenazol-3(2H)-ones obtained by a modified procedure involving the improved synthesis and isolation of the diseleno bis(dibenzoic) acid. The most efficient peroxide scavengers, N-bornyl and N-leucine methyl ester benzisoselenazol-3(2H)-ones, were further evaluated as cytotoxic agents on four cancer cell lines (MCF-7, HEP G2, HL 6, and DU 145) and normal cell line PNT1A. The highest antiproliferative potential was evaluated for two compounds bearing a 3-methylbutyl carbon chain, N-leucine methyl ester and N-3-methylbutyl benzisoselenazol-3(2H)-ones.

Keywords: antioxidant activity; biological activity; organoselenium compounds; terpenes.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antioxidants / chemical synthesis*
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Azoles / chemistry
  • Catalysis
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Isoindoles
  • MCF-7 Cells
  • Molecular Structure
  • Organic Chemicals
  • Organoselenium Compounds / chemical synthesis*
  • Organoselenium Compounds / chemistry
  • Organoselenium Compounds / pharmacology
  • Thiazoles / chemical synthesis*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Azoles
  • Isoindoles
  • Organic Chemicals
  • Organoselenium Compounds
  • Thiazoles
  • ebselen