2. Academic Validation
  3. Ruthenium(II)-Tris-pyrazolylmethane Complexes Inhibit Cancer Cell Growth by Disrupting Mitochondrial Calcium Homeostasis

Ruthenium(II)-Tris-pyrazolylmethane Complexes Inhibit Cancer Cell Growth by Disrupting Mitochondrial Calcium Homeostasis

  • J Med Chem. 2022 Aug 11;65(15):10567-10587. doi: 10.1021/acs.jmedchem.2c00722.
Jakub Cervinka 1 2,  Alberto Gobbo 3 4,  Lorenzo Biancalana 3,  Lenka Markova 1,  Vojtech Novohradsky 1,  Massimo Guelfi 3,  Stefano Zacchini 4,  Jana Kasparkova 1 5,  Viktor Brabec 1,  Fabio Marchetti 3
Affiliations

Affiliations

  • 1 Czech Academy of Sciences, Institute of Biophysics, Kralovopolska 135, CZ-61265 Brno, Czech Republic.
  • 2 Faculty of Science, Department of Biochemistry, Masaryk University, Kamenice 5, CZ-62500 Brno, Czech Republic.
  • 3 Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, I-56124 Pisa, Italy.
  • 4 Department of Industrial Chemistry "Toso Montanari", University of Bologna, Viale Risorgimento 4, I-40136 Bologna, Italy.
  • 5 Faculty of Science, Department of Biophysics, Palacky University in Olomouc, Slechtitelu 27, CZ-78371 Olomouc, Czech Republic.
PMID: 35913426 DOI: 10.1021/acs.jmedchem.2c00722
Abstract

While ruthenium arene complexes have been widely investigated for their medicinal potential, studies on homologous compounds containing a tridentate tris(1-pyrazolyl)methane ligand are almost absent in the literature. Ruthenium(II) complex 1 was obtained by a modified reported procedure; then, the reactions with a series of organic molecules (L) in boiling alcohol afforded novel complexes 2-9 in 77-99% yields. Products 2-9 were fully structurally characterized. They are appreciably soluble in water, where they undergo partial chloride/water exchange. The antiproliferative activity was determined using a panel of human Cancer cell lines and a noncancerous one, evidencing promising potency of 1, 7, and 8 and significant selectivity toward Cancer cells. The tested compounds effectively accumulate in Cancer cells, and mitochondria represent a significant target of biological action. Most notably, data provide convincing evidence that the mechanism of biological action is mediated by the inhibiting of mitochondrial calcium intake.

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