Combining anti-cancer drugs with artificial sweeteners: synthesis and anti-cancer activity of saccharinate (sac) and thiosaccharinate (tsac) complexes cis-[Pt(sac)2(NH3)2] and cis-[Pt(tsac)2(NH3)2]

J Inorg Biochem. 2014 Dec:141:55-57. doi: 10.1016/j.jinorgbio.2014.07.017. Epub 2014 Aug 1.

Abstract

The new platinum(II) complexes cis-[Pt(sac)2(NH3)2] (sac=saccharinate) and cis-[Pt(tsac)2(NH3)2] (tsac=thiosaccharinate) have been prepared, the X-ray crystal structure of cis-[Pt(sac)2(NH3)2] x H2O reveals that both saccharinate anions are N-bound in a cis-arrangement being inequivalent in both the solid-state and in solution at room temperature. Preliminary anti-cancer activity has been assessed against A549 human alveolar type-II like cell lines with the thiosaccharinate complex showing good activity.

Keywords: Ammine; Anti-cancer; Cisplatin; Saccharinate; Thiosaccharinate; X-ray structure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Coordination Complexes / chemical synthesis*
  • Coordination Complexes / pharmacology
  • Crystallography, X-Ray
  • Humans
  • Methotrexate / pharmacology
  • Organoplatinum Compounds / chemical synthesis*
  • Organoplatinum Compounds / pharmacology
  • Saccharin / analogs & derivatives
  • Saccharin / chemical synthesis*
  • Saccharin / pharmacology
  • Structure-Activity Relationship
  • Sweetening Agents / chemical synthesis*
  • Sweetening Agents / pharmacology

Substances

  • Antineoplastic Agents
  • Coordination Complexes
  • Organoplatinum Compounds
  • Sweetening Agents
  • Saccharin
  • Methotrexate