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Structure−activity relationships for cytotoxic ruthenium(II) arene complexes containing N,N-, N,O-, and O,O-chelating ligands
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Habtemariam, Abraha, Melchart, Michael, Fernández, Rafael, Parsons, Simon, Oswald, Iain D. H., Parkin, Andrew, Fabbiani, Francesca P. A., Davidson, James E., Dawson, Alice, Aird, Rhona E., Jodrell, Duncan I. and Sadler, P. J. (2006) Structure−activity relationships for cytotoxic ruthenium(II) arene complexes containing N,N-, N,O-, and O,O-chelating ligands. Journal of Medicinal Chemistry, Volume 49 (Number 23). pp. 6858-6868. doi:10.1021/jm060596m ISSN 0022-2623.
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Official URL: http://dx.doi.org/10.1021/jm060596m
Abstract
We report structure−activity relationships for organometallic RuII complexes of the type [(η6-arene)Ru(XY)Cl]Z, where XY is an N,N- (diamine), N,O- (e.g., amino acidate), or O,O- (e.g., β-diketonate) chelating ligand, the arene ranges from benzene derivatives to fused polycyclic hydrocarbons, and Z is usually PF6. The X-ray structures of 13 complexes are reported. All have the characteristic “piano-stool” geometry. The complexes most active toward A2780 human ovarian cancer cells contained XY = ethylenediamine (en) and extended polycyclic arenes. Complexes with polar substituents on the arene or XY = bipyridyl derivatives exhibited reduced activity. The activity of the O,O-chelated complexes depended strongly on the substituents and on the arene. For arene = p-cymene, XY = amino acidate complexes were inactive. Complexes were not cross-resistant with cisplatin, and cross-resistance to Adriamycin was circumvented by replacing XY = en with 1,2-phenylenediamine. Some complexes were also active against colon, pancreatic, and lung cancer cells.
Item Type: | Journal Article | ||||
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Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | ||||
Journal or Publication Title: | Journal of Medicinal Chemistry | ||||
Publisher: | American Chemical Society | ||||
ISSN: | 0022-2623 | ||||
Official Date: | 16 November 2006 | ||||
Dates: |
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Volume: | Volume 49 | ||||
Number: | Number 23 | ||||
Page Range: | pp. 6858-6868 | ||||
DOI: | 10.1021/jm060596m | ||||
Status: | Peer Reviewed | ||||
Publication Status: | Published | ||||
Access rights to Published version: | Restricted or Subscription Access |
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