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Anticancer water-soluble organoruthenium complexes: synthesis and preclinical evaluation

Pitto-Barry, Anaïs
; 
Azmanova, Maria
; 
Rafols, Laia
; 
Cooper, Patricia A.
; 
Seaton, Colin C.
; 
Publication Date
2022-09
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Keywords
Half-sandwich complexes, Bioinorganic chemistry, Phosphine ligands, Metallodrugs, In vivo evaluation
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© 2022 The Authors. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
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openAccess
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2022-07-14
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Abstract
The synthesis, characterisation, and evaluation of the in vitro cytotoxicity of five maleonitriledithiolate-based ruthenium metal complexes bearing various phosphine ligands towards two ovarian cancer cell lines (A2780 and A2780cisR), one non-small-cell lung cancer cell line (H460) and one normal prostate cell line (PNT2) are presented herein. These 18-electron complexes were designed with four water-soluble phosphine ligands to increase the water-solubility character of the corresponding electron-deficient ruthenium complex which showed great in vitro promises, and triphenylphosphine for comparison. The complexes with triphenylphosphine-3,3',3''trisulfonic acid and triphenylphosphine present similar cytotoxicity compared to the 16-electron precursor, with equal cytotoxicity to both A2780 and A2780cisR. Hints at the mechanism of action suggest an apoptotic pathway based on ROS production. No toxicity was observed in preliminary in vivo pilot studies for these two complexes in subcutaneous A2780 and A2780cisR xenograft models, with some evidence of tumour growth delay.
URI
http://hdl.handle.net/10454/19068
Version
Published version
Citation
Pitto-Barry A, Azmanova M, Rafols L et al (2022) Anticancer water-soluble organoruthenium complexes: synthesis and preclinical evaluation. ChemBioChem. 23(18): e202200259.
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https://doi.org/10.1002/cbic.202200259
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Article
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