Add time:09/28/2019         Source:sciencedirect.com

The synthesis is reported of the complexes [Rh- (CH3CO2)2L]2 where L = misonidazole, desmethylmisonidazole, 2-nitroimidazole-l-ethanol and 1-(2- hydroxy 3-methoxypropyl)-2-methyl-5-nitroimidazole (Roll-3696), and of the rhodium(II) butyrate analogues with the last two nitroimidazole ligands Crystals of [Rh(CH3CO2)2(Roll-3696)]2 are triclinic P1 with a = 7.982(2), b = 8.121(3), c = 13.327(3) Å, α = 77.23(2), β = 82.47(2), γ = 87.74(2)°, Z = 1. The structure was refined on 1833 reflections to R = 0.031. The molecule has the standard rhodium(II) acetate dinuclear structure with Rh-Rh = 2.399 Å, and with the ligand Roll-3696 coordinated to rhodium in terminal positions via N3 of the imidazole ring (Rh-N = 2.248 Å). The rhodium(II) carboxylate complexes with misonidazole, desmethylmisonidazole and Roll-3696 were examined for their ability to act as radiosensitizers of Chinese hamster mammalian cells in vitro. The rhodium(II) butyrate complex is substantially more toxic than the corresponding acetate and showed no sensitization at non-toxic concentrations. However, the acetates do sensitize and are up to 50X more efficient than the corresponding nitroimidazole ligand, when measured as the concentration required to give a similar increase in the radiation sensitivity of hypoxic cells. Some sensitization of aerobic cells is also observed but this is small compared to that seen under hypoxic conditions. The compounds containing the 2-nitroimidazole ligands are more efficient sensitizers than the complex containing the 5-nitroimidazole.

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