High mitochondrial accumulation of new gadolinium(III) agents within tumour cells

Chem Commun (Camb). 2014 Mar 4;50(18):2252-4. doi: 10.1039/c3cc46903d. Epub 2013 Dec 19.

Abstract

The first bifunctional Gd(III) complexes covalently bound to arylphosphonium cations and the first tumour-cell selective mitochondrial agents designed for potential application in binary cancer therapies are reported. The highest in vitro cellular uptake for any Gd complex reported to date is described, with levels exceeding 10(10) Gd atoms per tumour cell.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Gadolinium / chemistry
  • Gadolinium / metabolism
  • Gadolinium / pharmacology*
  • Humans
  • Mitochondria / chemistry
  • Mitochondria / drug effects*
  • Mitochondria / metabolism
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / metabolism
  • Organometallic Compounds / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Organometallic Compounds
  • Gadolinium