Biological activities of polypyridyl-type ligands: implications for bioinorganic chemistry and light-activated metal complexes

Austin C. Hachey, Dmytro Havrylyuk, Edith C. Glazer

Research output: Contribution to journalReview articlepeer-review

35 Scopus citations

Abstract

Polypyridyl coordinating ligands are common in metal complexes used in medicinal inorganic chemistry. These ligands possess intrinsic cytotoxicity, but detailed data on this phenomenon are sparse, and cytotoxicity values vary widely and are often irreproducible. To provide new insights into the biological effects of bipyridyl-type ligands and structurally related metal-binding systems, reports of free ligand cytotoxicity were reviewed. The cytotoxicity of 25 derivatives of 2,2′-bipyridine and 1,10-phenanthroline demonstrates that there is no correlation between IC50 values and ligand properties such as pKa, log D, polarizability volume, and electron density, as indicated by NMR shifts. As a result of these observations, as well as the various reported mechanisms of action of polypyridyl ligands, we offer the hypothesis that biological effects are governed by the availability of and affinity for specific metal ions within the experimental model.

Original languageEnglish
Pages (from-to)191-202
Number of pages12
JournalCurrent Opinion in Chemical Biology
Volume61
DOIs
StatePublished - Apr 2021

Bibliographical note

Publisher Copyright:
© 2021 Elsevier Ltd

Keywords

  • 1,10-Phenanthroline
  • Chemotherapy
  • Copper
  • Iron
  • Ligand
  • Natural products
  • Polypyridyl
  • Ruthenium

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry

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