Palladium(ii) complexes with thiosemicarbazones derived from pyrene as topoisomerase IB inhibitors

Dalton Trans. 2019 Nov 12;48(44):16509-16517. doi: 10.1039/c9dt02570g.

Abstract

New palladium complexes with thiosemicarbazonate ligands derived from pyrene exhibit potent antiproliferative activity against A2780 and cisplatin-resistant A2780Cis human ovarian cancer cells, which is dependent on substituent groups of the thiosemicarbazone ligands. Cellular accumulation and distribution studies confirmed that palladium enters the cell nucleus. DNA and topoisomerase IB studies show that one complex is a potent TopIB inhibitor, with selectivity for cancer versus normal cells.

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cisplatin / pharmacology
  • Coordination Complexes / chemistry*
  • Coordination Complexes / pharmacology
  • Drug Resistance, Neoplasm
  • Humans
  • Kinetics
  • Palladium / chemistry*
  • Pyrenes / chemistry*
  • Thiosemicarbazones / chemistry*
  • Topoisomerase Inhibitors / chemistry*
  • Topoisomerase Inhibitors / pharmacology

Substances

  • Antineoplastic Agents
  • Coordination Complexes
  • Pyrenes
  • Thiosemicarbazones
  • Topoisomerase Inhibitors
  • Palladium
  • Cisplatin