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Digital archive of theses discussed at the University of Pisa

 

Thesis etd-01102018-150916


Thesis type
Tesi di dottorato di ricerca
Author
BIANCALANA, LORENZO
URN
etd-01102018-150916
Thesis title
Synthesis, Characterization and Cytotoxicity of New Ruthenium(II) Arene Compounds as Potential Anticancer Drugs
Academic discipline
CHIM/03
Course of study
SCIENZE CHIMICHE E DEI MATERIALI
Supervisors
tutor Prof. Marchetti, Fabio
Keywords
  • anticancer
  • arene compounds
  • bioactive molecule
  • cytotoxicity
  • metal-based drugs
  • Ruthenium
Graduation session start date
15/02/2018
Availability
Full
Summary
The work carried out on this Thesis was aimed to the preparation of new Ruthenium(II) arene compounds and a preliminary investigation of their antiproliferative activity. Inspired by the promising RAPTA and RAED-type complexes, structurally-related Ru compounds with arylphosphines and α-diimines ligands were considered. Moreover, on the light of antitumour effects exerted by some α-amino acid and controversial biological results in the literature on related Ruthenium(II)-arene complexes, this type of compounds was also investigated. The functionalization of the resulting Ru complexes containing arylphosphines, α-amino acids or α-diimines ligands with bioactive molecules was applied as a general strategy to improve the biological properties. Ethacrynic acid, Aspirin, Diclofenac, dichloroacetic acid, Ibuprofen, Indomethacin and valproic acid were selected for this purpose for their known antitumour effects mainly associated to the inhibition of specific enzymes involved in cancer cell growth. The newly-synthesized compounds were fully characterized (analytical and spectroscopic techniques, X-ray diffraction) and their stability in aqueous media was assessed. Selected Ruthenium complexes were studied for their antiproliferative activity in vitro against human ovarian (A2780/A2780cisR), pancreatic (BxPC3) and breast (MDA-MB-231) cancer cells lines, and towards non-cancerous cell lines as a comparison. The results herein presented delineated the anticancer potential of these three types of Ru(II)-arene compounds and will be a useful feedback for the design of second generation of compounds.
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