Luminescent cyclometalated platinum(II) complexes with amino acid ligands for protein binding

Chem Commun (Camb). 2005 Feb 28:(8):1025-7. doi: 10.1039/b414936j. Epub 2005 Jan 5.

Abstract

Pt(C/N)(phe)(1, C/N = 2-(2'-thienyl)pyridine, phe = phenylalanine) shows a high binding affinity (ca. 10(6) dm(3) mol(-1)) and selectivity towards human serum albumin (HSA) and such binding is accompanied by an enhancement of photoluminescence at 562 nm; both the protein binding affinity and cytotoxicities of [Pt(C/N)(phe)(1), Pt(C/N)(trp)(2, trp = tryptophan) and Pt(C/N)(gly)(3, gly = glycine)] are affected by the amino acid ligand with having an IC(50) of up to 1 microM against a number of carcinoma cell lines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemistry*
  • Amino Acids / metabolism*
  • Cell Line, Tumor
  • Cyclization
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • Humans
  • Inhibitory Concentration 50
  • Ligands
  • Luminescent Agents / chemistry*
  • Luminescent Agents / metabolism
  • Luminescent Measurements
  • Molecular Structure
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / metabolism
  • Organometallic Compounds / pharmacology
  • Platinum / chemistry*
  • Platinum / metabolism
  • Protein Binding
  • Serum Albumin / chemistry*
  • Serum Albumin / metabolism
  • Structure-Activity Relationship

Substances

  • Amino Acids
  • Ligands
  • Luminescent Agents
  • Organometallic Compounds
  • Serum Albumin
  • Platinum