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dc.contributor.author
Weiss, Andrea
dc.contributor.author
Berndsen, Robert H.
dc.contributor.author
Dubois, Maxime
dc.contributor.author
Müller, Cristina
dc.contributor.author
Schibli, Roger
dc.contributor.author
Griffioen, Arjan W.
dc.contributor.author
Dyson, Paul J.
dc.contributor.author
Nowak-Sliwinska, Patrycja
dc.date.accessioned
2019-06-18T14:24:19Z
dc.date.available
2017-06-11T13:22:05Z
dc.date.available
2019-06-18T14:24:19Z
dc.date.issued
2014-12-01
dc.identifier.issn
2041-6520
dc.identifier.issn
2041-6539
dc.identifier.other
10.1039/c4sc01255k
en_US
dc.identifier.uri
http://hdl.handle.net/20.500.11850/91557
dc.identifier.doi
10.3929/ethz-b-000091557
dc.description.abstract
Based on the clinical success of platinum-based anti-cancer drugs such as cisplatin, carboplatin and oxaliplatin, a variety of other metal-based anti-cancer compounds are being investigated. In particular, a number of ruthenium-based compounds have been identified which exhibit unique biochemical properties and reduced toxicity profiles compared to the clinically used platinum-based drugs. We have developed a series of organometallic ruthenium(II)-arene complexes that were shown to exert anti-metastatic activity with relatively minor activity on primary tumor growth. Here, we show that the prototype compound, [Ru(η6-p-cymene)Cl2(pta)], where pta = 1,3,5-triaza-7-phosphaadamantane (RAPTA-C), reduces the growth of primary tumors in preclinical models for ovarian and colorectal carcinomas. When administered daily at relatively low doses (0.2 mg kg−1), RAPTA-C was shown to significantly reduce the growth of the A2780 ovarian carcinoma transplanted onto the chicken chorioallantoic membrane model. Similar activity was observed in LS174T colorectal carcinoma in athymic mice, albeit at a higher dose. In both models, a clear inhibition of microvessel density was observed, confirming the previously discovered anti-angiogenic mechanism of RAPTA-C. Biodistribution studies with radiolabeled (103Ru) RAPTA-C indicate that the compound is rapidly cleared from the organs and the bloodstream through excretion by the kidneys. As such, RAPTA-C is a promising compound for translation to clinical evaluation.
en_US
dc.format
application/pdf
en_US
dc.language.iso
en
en_US
dc.publisher
Royal Society of Chemistry
en_US
dc.rights.uri
http://creativecommons.org/licenses/by/3.0/
dc.title
In vivo anti-tumor activity of the organometallic ruthenium(II)-arene complex [Ru(η6-p-cymene)Cl2(pta)] (RAPTA-C) in human ovarian and colorectal carcinomas
en_US
dc.type
Journal Article
dc.rights.license
Creative Commons Attribution 3.0 Unported
dc.date.published
2014-08-05
ethz.journal.title
Chemical Science
ethz.journal.volume
5
en_US
ethz.journal.issue
12
en_US
ethz.journal.abbreviated
Chem. Sci.
ethz.pages.start
4742
en_US
ethz.pages.end
4748
en_US
ethz.version.deposit
publishedVersion
en_US
ethz.identifier.wos
ethz.identifier.scopus
ethz.identifier.nebis
006104946
ethz.publication.place
Cambridge
en_US
ethz.publication.status
published
en_US
ethz.date.deposited
2017-06-11T13:22:32Z
ethz.source
ECIT
ethz.identifier.importid
imp59365276c340c20529
ethz.ecitpid
pub:143938
ethz.eth
yes
en_US
ethz.availability
Open access
en_US
ethz.rosetta.installDate
2017-07-14T17:47:33Z
ethz.rosetta.lastUpdated
2022-03-28T23:06:44Z
ethz.rosetta.versionExported
true
ethz.COinS
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