4.7 Article

Cationic carboxylate and thioacetate ruthenium(II) complexes: synthesis and cytotoxic activity against anaplastic thyroid cancer cells

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DALTON TRANSACTIONS
卷 49, 期 24, 页码 8375-8388

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d0dt01390k

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  1. Ministero dell'Universita e della Ricerca (MIUR), PRIN 2015 program [20154X9ATP_005]
  2. University of Udine

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The cationic acetate ruthenium complex [Ru(eta(1)-OAc)(CO)(dppb)(phen)]OAc (1) is easily prepared in 83% yield from [Ru(eta(1)-OAc)(eta(2)-OAc)(CO)(dppb)] (dppb = 1,4-bis(diphenylphosphino)butane) and 1,10-phenanthroline (phen) in MeOH. The derivative1undergoes easy substitution of the coordinated acetate by reaction with NaOPiv, KSAc, and KSCN in MeOH, affording the corresponding complexes [RuX(CO)(dppb)(phen)]X (X = OPiv,2; SAc,3; and NCS,4), whereas its reaction with NaCl and NH(4)PF(6)affords [RuCl(CO)(dppb)(phen)]PF6(5). Carboxylate complexes1and2show high solubility in water, enabling easy exchange of the coordinated carboxylate by water and other ligands (CH3CN, glutathione). Cationic complexes1-5, compared to Cisplatin, display a strong cell viability decrease in two human anaplastic thyroid cancer cell lines (SW1736 and 8505C), ranging from 3.10 mu M to 0.09 mu M EC(50)values. The most active compounds1-3show a marked increment of apoptosis and decrease of cancer cell aggressiveness, making them promising candidates for further evaluation studies.

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