1 research outputs found
Organometallic Glutathione <i>S</i>‑Transferase Inhibitors
A new
family of organometallic <i>p</i>-cymene rutheniumÂ(II)
and osmiumÂ(II) complexes conjugated to ethacrynic acid, a glutathione
transferase (GST) inhibitor, is reported. The ethacrynic acid moiety
(either one or two) is tethered to the arene rutheniumÂ(II) and osmiumÂ(II)
fragments via strongly coordinating modified bipyridine ligands. The
solid-state structure of one of the complexes, i.e. [OsÂ(η<sup>6</sup>-<i>p</i>-cymene)ÂCl]Â[(4′-methyl-[2,2′-bipyridin]-4-yl)Âmethyl-2-(2,3-dichloro-4-(2-methylenebutanoyl)Âphenoxy)Âacetate]ÂCl,
was established by single-crystal X-ray diffraction, corroborating
the expected structure. The complexes are efficient inhibitors of
GST P1-1, an enzyme expressed in cancer cells and implicated in drug
resistance, and are cytotoxic to the GST-overexpressing chemoresistant
A2780cisR ovarian cancer cell line