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Ruthenium(II) Complex with 1-Hydroxy-9,10-Anthraquinone Inhibits Cell Cycle Progression at G0/G1 and Induces

Júlia S M Dias1, Guilherme A Ferreira-Silva2, Rommel B Viana3

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Ruthenium complexes with anthraquinone derivatives show potential against melanoma. Complex (1) effectively inhibits melanoma cell proliferation and induces apoptosis, offering a promising new therapeutic avenue.

Keywords:
1-hydroxy-9,10-anthraquinoneantiproliferative activitymelanomaruthenium complexes

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Area of Science:

  • Inorganic Chemistry
  • Medicinal Chemistry
  • Materials Science

Background:

  • Melanoma is an aggressive skin cancer.
  • Ruthenium complexes offer advantages over platinum drugs for cancer chemotherapy.
  • Anthraquinone derivatives have shown therapeutic potential, including in melanoma treatment.

Purpose of the Study:

  • Synthesize and characterize two novel ruthenium complexes incorporating 1-hydroxy-9,10-anthraquinone.
  • Evaluate the DNA-binding properties and cytotoxic activity of these complexes against human melanoma cell lines.

Main Methods:

  • Complex synthesis and characterization using spectroscopic (IR, UV-vis, NMR) and analytical techniques.
  • Single-crystal X-ray diffraction for structural determination of one complex.
  • DNA-binding studies and cytotoxicity assays (IC50) on melanoma cell lines.
  • Density Functional Theory (DFT) calculations.

Main Results:

  • Two ruthenium complexes, trans-[Ru(HQ)(PPh3)2(bipy)]PF6 (1) and cis-[RuCl2(HQ)(dppb)] (2), were successfully synthesized and characterized.
  • Complex (2) structure confirmed bidentate coordination of HQ. Both complexes interact with DNA via intercalation, electrostatic attraction, or hydrogen bonding.
  • Complex (1) exhibited significant cytotoxicity against CHL-1 melanoma cells (IC50 = 14.50 ± 1.09 µM).

Conclusions:

  • Ruthenium complex (1) demonstrates potent cytotoxic activity against melanoma cells.
  • Complex (1) inhibits cell proliferation and induces apoptosis, potentially through a pro-oxidant effect and cell cycle arrest.
  • These findings highlight the therapeutic potential of novel ruthenium-anthraquinone complexes in melanoma treatment.