Nowadays several metal compounds are widely used in medicine as therapeutic and diagnostic agents. Due to their versatile biochemical properties, ruthenium-based compounds have shown to be promising anti-cancer agents as alternative to cisplatin and its derivatives. [1] The aim of our work is to investigate the effects of new ruthenium(II) complexes of general formula [RuX(CO)(dppb)(phen)]X [X = acetate, pivalate, thioacetate; dppb = 1,4- bis(diphenylphosphino)butane; phen = 1,10-phenanthroline] [2] on two different types of anaplastic thyroid cancer cells, focusing our attention on the nature of the X group. Interestingly, these compounds are able to reach very low IC50 values after 72 h of incubation. In addition, the introduction of a chiral diphosphine, such as (R,R)- and (S,S)-Skewphos, leads to single enantiomers which show a marked difference in in vitro biological activity.

Chiral ruthenium complexes: synthesis and evaluation of their anticancer activity

Denise Lovison
;
Lorenzo Allegri;Giuseppe Damante;Walter Baratta
2019-01-01

Abstract

Nowadays several metal compounds are widely used in medicine as therapeutic and diagnostic agents. Due to their versatile biochemical properties, ruthenium-based compounds have shown to be promising anti-cancer agents as alternative to cisplatin and its derivatives. [1] The aim of our work is to investigate the effects of new ruthenium(II) complexes of general formula [RuX(CO)(dppb)(phen)]X [X = acetate, pivalate, thioacetate; dppb = 1,4- bis(diphenylphosphino)butane; phen = 1,10-phenanthroline] [2] on two different types of anaplastic thyroid cancer cells, focusing our attention on the nature of the X group. Interestingly, these compounds are able to reach very low IC50 values after 72 h of incubation. In addition, the introduction of a chiral diphosphine, such as (R,R)- and (S,S)-Skewphos, leads to single enantiomers which show a marked difference in in vitro biological activity.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11390/1171840
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