Cyclam-based polymeric copper chelators for gene delivery and potential PET imaging

Biomacromolecules. 2012 Oct 8;13(10):3220-7. doi: 10.1021/bm3009999. Epub 2012 Sep 25.


A series of reducible polycationic copper chelators (RPCs) based on 1,4,8,11-tetraazacyclotetradecane (cyclam) were synthesized by Michael addition. Molecular weight of the polycations was controlled by reaction stoichiometry and reaction conditions, resulting in polymers with molecular weights ranging from 4400 to 13 800. The cyclam moieties in the polycations retained their ability to form complexes with Cu(II). The presence of disulfide bonds in the polycations resulted in substantially lower cytotoxicity than control 25 kDa poly(ethyleneimine). RPC as well as their complexes with Cu(II) exhibited high transfection activity in vitro. The reported polycationic Cu(II) chelates represent promising nucleic acid delivery vectors with potential for future theranostic applications.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Chelating Agents / chemical synthesis
  • Chelating Agents / chemistry*
  • Copper / chemistry
  • Gene Transfer Techniques*
  • Genetic Vectors / chemical synthesis
  • Genetic Vectors / chemistry*
  • Hep G2 Cells
  • Heterocyclic Compounds / chemistry*
  • Humans
  • Molecular Structure
  • Polymers / chemistry*
  • Positron-Emission Tomography*
  • Tumor Cells, Cultured


  • Chelating Agents
  • Heterocyclic Compounds
  • Polymers
  • cyclam
  • Copper