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N-Heterocyclic Carbene–Polyethylenimine Platinum Complexes with Potent in Vitro and in Vivo Antitumor Efficacy

Authors
  • Chekkat, Neila
  • Georges Dahm
  • Chardon, Edith
  • Wantz, May
  • Sitz, Justine
  • Decossas, Marion
  • Lambert, Olivier
  • Frisch, Benoit
  • Rubbiani, Riccardo
  • Gasser, Gilles
  • Guichard, Gilles
  • Fournel, Sylvie
  • Bellemin-Laponnaz, Stéphane
Type
Published Article
Journal
Bioconjugate Chemistry
Publisher
American Chemical Society
Publication Date
Aug 06, 2016
Volume
27
Identifiers
DOI: 10.1021/acs.bioconjchem.6b00320
Source
MyScienceWork
License
White

Abstract

The current interest for platinum N-heterocyclic carbene complexes in cancer research stems from their impressive toxicity reported against a range of different human cancer cells. To date, the demonstration of their in vivo efficacy relative to that of established platinum-based drugs has not been specifically addressed. Here, we introduce an innovative approach to increase the NHC-Pt complex potency whereby multiple NHC-Pt(II) complexes are coordinated along a polyethylenimine polymer (PEI) chain. We show that such NHC-Pt(II)-PEI conjugates induce human cancer cell death in vitro and in vivo in a xenograft mouse model with no observable side effects in contrast to oxaliplatin. Additional studies indicate nucleus and mitochondria targeting and suggest various mechanisms of action compared to classical platinum-based anticancer drugs.

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