Antiproliferative activity of salinomycin and its derivatives

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7146-50. doi: 10.1016/j.bmcl.2012.09.068. Epub 2012 Sep 27.

Abstract

Antiproliferative activity of seven amides and one benzotriazole ester derivative of salinomycin, a polyether ionophore antibiotic, with recently reported antibacterial activity, are herein described. Salinomycin and the majority of derivatives exhibit potent antiproliferative activity against the drug-resistant cancer cell lines. Moreover almost all derivatives show stronger activity against LoVo/DX cell line than that of unmodified salinomycin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / toxicity
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Crystallography, X-Ray
  • Drug Resistance, Neoplasm / drug effects
  • HL-60 Cells
  • Humans
  • Molecular Conformation
  • Pyrans / chemical synthesis
  • Pyrans / chemistry*
  • Pyrans / toxicity
  • Structure-Activity Relationship
  • Triazoles / chemistry

Substances

  • Amides
  • Antineoplastic Agents
  • Pyrans
  • Triazoles
  • salinomycin
  • benzotriazole