Discovery of a (19)F MRI sensitive salinomycin derivative with high cytotoxicity towards cancer cells

Chem Commun (Camb). 2016 Apr 14;52(29):5136-9. doi: 10.1039/c6cc01508e. Epub 2016 Mar 21.

Abstract

Salinomycin is a promising anti-cancer agent which selectively targets cancer stem cells. To improve its potency and selectivity, an analog library of salinomycin was generated by site-specific modification and CuAAc derivatization. Through a cytotoxicity analysis of the library, a fluorinated analog with high potency, selectivity, and (19)F MRI sensitivity was discovered as a novel theranostic agent.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Crystallography, X-Ray
  • Halogenation
  • Humans
  • Magnetic Resonance Imaging*
  • Mice
  • Models, Molecular
  • Neoplasms / diagnostic imaging*
  • Neoplasms / drug therapy*
  • Pyrans / chemistry*
  • Pyrans / pharmacology*

Substances

  • Antineoplastic Agents
  • Pyrans
  • salinomycin