Acridine-containing RuII, OsII, RhIII and IrIII Half-Sandwich Complexes: Synthesis, Structure and Antiproliferative Activity

Asanda C. Matsheku, Marian Y.H. Chen, Sandra Jordaan, Sharon Prince, Gregory S. Smith, Banothile C.E. Makhubela

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)


Research aimed at enhancing the efficacy of organometallic complexes against cancer, has shown that attaching bio-active molecules to (metallo)drugs often enhances their biological properties. New salicylaldimine and 2-pyridylimine ligands (L2 and L3), containing a bio-active acridine scaffold, were synthesized and complexed to Rh(III), Ir(III), Ru(II) and Os(II) metal ion centers. The resulting acridine-containing half-sandwich complexes have been characterized fully by elemental analysis, FT-IR and NMR spectroscopy, HR-ESI mass spectrometry as well as single crystal X-ray diffraction, for the Rh(III) N^N bidentate complex [RhCp*Cl(L3)][BPh4]. The antiproliferative activity of the ligands (L2 and L3) and complexes (C1 to C9) were evaluated in vitro against human promyelocytic leukemia cells (HL60) and normal skin fibroblast cells (FG0). The compounds exhibit good activities against HL60 cells and are consistently selective towards cancerous cells over non-tumorous cells. This study demonstrates the potential of such hybrid compounds to target cancer cells specifically. The most active complex, [RhCp*Cl(L2)], exhibited binding to DNA model guanosine-5’-monophosphate (5’-GMP) which suggests a mode of action involving interaction of the complex with 5’-GMP found on DNA backbone.

Original languageEnglish
Article numbere3852
JournalApplied Organometallic Chemistry
Issue number12
Publication statusPublished - Dec 2017


  • acridine derivatives
  • anticancer agents
  • antiproliferative activity
  • bioorganometallic chemistry
  • half-sandwich complexes

ASJC Scopus subject areas

  • General Chemistry
  • Inorganic Chemistry


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