Due to the severe toxicity of anticancer platinum complexes and acquired drug resistance, research has focused on arene ruthenium complexes as viable alternatives. Arene complexes of the formula [areneRu(μ2-L)Cl]2 and (areneRu)2(μ2-L)3+ (L = phenyl thiolate) are known to be cytotoxic with IC50 values in the micromolar and submicromolar ranges, respectively. We have incorporated glucose ligands into arene-ruthenium complexes to investigate whether glucose confers specificity for cancerous cells over normal cells. Reaction of the sodium salt of β-D-thioglucose with [cymeneCl2Ru]2 forms [(cymene)Ru(μ2-thioglucose)]2 (1) and [(cymeneRu)2(μ2-thioglucose)3]Cl (2). Compound 1 was successfully purified by HPLC and characterized by ESI-MS and NMR. Growth assays were performed in a somatic line (HUVEC), a breast cancer line (T47D), and a cisplatin-resistant ovarian cancer cell line (A2780cis). Fluorescence staining of treated T47D and A2780cis cells indicates that morphological changes in actin increase with higher concentrations. Wound assays in T47D cells indicate a dose-dependent inhibition of motility after treatment.

Glycoconjugates of organometallic ruthenium-arene complexes

253rd National Meeting (2017)

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