<p>An approach was developed to the synthesis of two types of binuclear Pt<sup>II</sup> complexes: complexes with azaheterocyclic carrier ligands based on imidazole as a linker and iodide anions as leaving groups, and complexes based on pyromellitic acid as a ligand, acting as a linker and a leaving group, and a pyrazole moiety as a carrier ligand. The antiproliferative activity of both mononuclear and binuclear complexes based on monodentate pyrazoles was found to depend on a combination of substituents at the pyrazole nitrogen atom and the nature of the leaving group. Binuclear Pt<sup>II</sup> complexes with alkyl-1<i>H</i>-pyrazoles as carrier ligands exhibit high activity in the A2780C is cisplatin-resistant cell line.</p>

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Azaheterocycles in the design of novel binuclear PtII complexes

  • A. S. Pavlova,
  • I. A. Likhachev,
  • A. M. Vasileva,
  • N. E. Borisova,
  • A. A. Nazarov,
  • A. A. Antonets,
  • A. V. Mironov,
  • I. A. Rodin,
  • Y. V. Timchenko,
  • T. A. Podrugina

摘要

An approach was developed to the synthesis of two types of binuclear PtII complexes: complexes with azaheterocyclic carrier ligands based on imidazole as a linker and iodide anions as leaving groups, and complexes based on pyromellitic acid as a ligand, acting as a linker and a leaving group, and a pyrazole moiety as a carrier ligand. The antiproliferative activity of both mononuclear and binuclear complexes based on monodentate pyrazoles was found to depend on a combination of substituents at the pyrazole nitrogen atom and the nature of the leaving group. Binuclear PtII complexes with alkyl-1H-pyrazoles as carrier ligands exhibit high activity in the A2780C is cisplatin-resistant cell line.