Arene ruthenium dithiolato-carborane complexes for boron neutron capture therapy (BNCT)

作者：Romero Canelon Isolda; Phoenix Ben; Pitto Barry Anais; Johanna Tran; Soldevila Barreda Joan J; Kirby Nigel; Green Stuart^*; Sadler Peter J; Barry Nicolas P E

来源：Journal of Organometallic Chemistry, 2015, 796: 17-25.

DOI：10.1016/j.jorganchem.2015.05.011

• Arene ruthenium
• Carborane
• Pluronic
• Micelles
• Boron neutron capture therapy

We report the effect of low-energy thermal neutron irradiation on the antiproliferative activities of a highly hydrophobic organometallic arene ruthenium dithiolato-carborane complex [Ru(p-cymene) (1,2dicarba-closo-dodecarborane-1,2-dithiolato)] (1), and of its formulation in Pluronic (R) triblock copolymer P123 core-shell micelles (RuMs). Complex 1 was highly active, with and without neutron irradiation, towards human ovarian cancer cells (A2780; IC50 0.14 mu M and 0.17 mu M, respectively) and cisplatin-resistant human ovarian cancer cells (A2780cisR; IC50 0.05 and 0.13 mu M, respectively). Complex 1 was particularly sensitive to neutron irradiation in A2780cisR cells (2.6 x more potent after irradiation compared to non-irradiation). Although less potent, the encapsulated complex 1 as RuMs nanoparticles resulted in higher cellular accumulation (2.5x), and was sensitive to neutron irradiation in A2780 cells (1.4x more potent upon irradiation compared to non-irradiation).

• 出版日期2015-11-1