Vanadium (V) catecholate complexes are cytotoxic and highly selective for cancerous tissue, and might be effective for treating cancer. Early attempts in the development of these complexes, such as [VO(HSHED)cat], have shown limited success due to rapid hydrolysis and degradation. It was hypothesized that increased hydrophobicity and steric hinderance of the complex would slow the rate of hydrolysis and degradation, leading to increased efficacy. Substitution of starting materials with similar compounds, decorated with one or more tert-butyl groups, resulted in vanadium (V) complexes, such as [VO(HSHED)dtb], with greater hydrophobicity and steric hinderance, and extended lifetimes in both DMSO/water solutions, as well as cell culture medium. These compounds were characterized by 1H NMR, 13C NMR, and 51V NMR, mass spectrometry, and UV-Vis. The efficacy of these compounds as chemotherapeutics was confirmed by testing on cancer lines, including T98g, an aggressive form of glial-cell cancer. It was found that greater steric hindrance and hydrophobicity lead to slower hydrolytic degradation which increased the efficacy of [VO(HSHED)dtb]. As a result of the heightened efficacy of [VO(HSHED)dtb],we have worked to develop compounds with greater steric bulk and in larger quantities for animal testing.

Sterically hindered hydrophobic vanadium(V) complexes as chemotherapeutics

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