Organometallic Osmium Arene Complexes with Potent Cancer Cell Cytotoxicity

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• 作者：Ying Fu ; Abraha Habtemariam ; Ana M. Pizarro ; Sabine H. van Rijt ; David J. Healey ; Patricia A. Cooper ; Steven D. Shnyder ; Guy J. Clarkson ; Peter J. Sadler
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：November 25, 2010
• 年：2010
• 卷：53
• 期：22
• 页码：8192-8196
• 全文大小：799K
• 年卷期：v.53,no.22(November 25, 2010)
• ISSN：1520-4804

文摘

Iodido osmium(II) complexes [Os(η⁶-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., IC₅₀ = 140 nM for [Os(η⁶-bip)(azpy-NMe₂)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.