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Organometallic osmium arene complexes with potent cancer cell cytotoxicity
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Fu, Y. (Ying), Habtemariam, Abraha, Pizarro, Ana M., Rijt, Sabine H. van, Healey, David J., Cooper, Patricia A., Shnyder, Steven D., Clarkson, Guy J. and Sadler, P. J. (2010) Organometallic osmium arene complexes with potent cancer cell cytotoxicity. Journal of Medicinal Chemistry, Vol.53 (No.22). pp. 8192-8196. doi:10.1021/jm100560f ISSN 0022-2623.
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Official URL: http://dx.doi.org/10.1021/jm100560f
Abstract
Iodido osmium(II) complexes [Os(eta(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., IC50 = 140 nM for [Os(eta(6)-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 or, broad therapeutic window. The most active complexes are stable and inert toward aquation. Their cytotoxic activity appears to involve redox mechanisms.
| Item Type: | Journal Article | ||||
|---|---|---|---|---|---|
| Subjects: | Q Science > QD Chemistry Q Science > QP Physiology |
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| Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | ||||
| Library of Congress Subject Headings (LCSH): | Organometallic compounds -- Therapeutic use, Aromatic compounds -- Therapeutic use, Osmium compounds -- Therapeutic use, Cell-mediated cytotoxicity | ||||
| Journal or Publication Title: | Journal of Medicinal Chemistry | ||||
| Publisher: | American Chemical Society | ||||
| ISSN: | 0022-2623 | ||||
| Official Date: | 25 November 2010 | ||||
| Dates: |
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| Volume: | Vol.53 | ||||
| Number: | No.22 | ||||
| Number of Pages: | 5 | ||||
| Page Range: | pp. 8192-8196 | ||||
| DOI: | 10.1021/jm100560f | ||||
| Status: | Peer Reviewed | ||||
| Publication Status: | Published | ||||
| Access rights to Published version: | Restricted or Subscription Access | ||||
| Funder: | Medical Research Council (Great Britain) (MRC), Engineering and Physical Sciences Research Council (EPSRC), Birmingham Science City, European Regional Development Fund (ERDF), Advantage West Midlands (AWM) |
Data sourced from Thomson Reuters' Web of Knowledge
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