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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

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Official URL: http://dx.doi.org/10.1021/jm100560f

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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
Divisions: Faculty of 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:
DateEvent
25 November 2010Published
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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