Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry, CV4 7AL, UK.
J Med Chem. 2010 Nov 25;53(22):8192-6. doi: 10.1021/jm100560f. Epub 2010 Oct 26.
Iodido osmium(II) complexes Os(η(6)-arene)(XY)I (XY = p-hydroxy or p-dimethylaminophenylazopyridine, arene = p-cymene or biphenyl) are potently cytotoxic at nanomolar concentrations toward a panel of human cancer cell lines; e.g., IC(50) = 140 nM for Os(η(6)-bip)(azpy-NMe(2))I toward A2780 ovarian cancer cells. They exhibit low toxicity and negligible deleterious effects in a colon cancer xenograft model, giving rise to the possibility of a broad therapeutic window. The most active complexes are stable and inert toward aquation. Their cytotoxic activity appears to involve redox mechanisms.
碘代锇（II）配合物Os(η(6)-芳烃)(XY)I（XY = 对羟基或对二甲氨基苯偶氮吡啶，芳烃 = 对伞花烃或联苯）在纳摩尔浓度下对一系列人类癌细胞系具有很强的细胞毒性；例如，Os(η(6)-联苯)(azpy-NMe(2))I对 A2780 卵巢癌细胞的 IC(50)为 140 nM。它们在结肠癌异种移植模型中表现出低毒性和可忽略的有害影响，这为广泛的治疗窗提供了可能性。最活跃的配合物是稳定和惰性的水合。它们的细胞毒性活性似乎涉及氧化还原机制。
