Evaluation of trimetallic Ru(II)- and Os(II)-Arene complexes as potential anticancer agents

Banothile C.E. Makhubela, Mervin Meyer, Gregory S. Smith

Research output: Contribution to journalArticlepeer-review

32 Citations (Scopus)

Abstract

Schiff-base ligands, tris-2-(salicylaldimine ethyl)amine and tris-2-(2-pyridylimine ethyl)amine (1 and 2) were prepared and complexed to Ru(II) and Os(II) entities to form new trimetallic complexes (3-10). The complexes are air- and moisture-stable and have been characterized fully using elemental analysis, FT-IR and NMR spectroscopy as well as HR-ESI-TOF-MS spectrometry. Related mononuclear analogues (11-14) were also prepared via the Schiff-base condensation reaction of propyl amine and the appropriate aldehyde to form propysalicylaldimine and propyl-2-pyridylimine ligands. Upon complexation with the respective metal dimers, ([OsCl2(p-cym)]2 and [OsBr2(p-cym)]2) complexes (11-14) formed and were characterized by elemental analysis, NMR, FT-IR spectroscopy and mass spectrometry. The cytotoxicity of the trimetallic complexes (3-10) and their mononuclear analogues were established against human osteosarcoma (MG63), human ovarian (A2780cisR; cisplatin-resistant) cancer cells and model human non-cancerous cells (KMST6, fibroblast). All the complexes exhibited moderate to high anti-cancer activities and the most potent complexes were further evaluated for their ability to inhibit DNA topoisomerase I (Topo I) - an enzyme key to cellular genetic processes, such as DNA replication and transcription.

Original languageEnglish
Pages (from-to)229-241
Number of pages13
JournalJournal of Organometallic Chemistry
Volume772-773
DOIs
Publication statusPublished - 1 Dec 2014
Externally publishedYes

Keywords

  • Cancer
  • Cytotoxicity
  • I
  • Ruthenium(II)-arenes and osmium(II)-arenes
  • Topoisomerase
  • Trimetallic

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry
  • Materials Chemistry

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