Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity

dc.contributor.authorHorvath, Ulrike E.I.
dc.contributor.authorDobrzanska, Liliana
dc.contributor.authorStrasser, Christoph E.
dc.contributor.authorBouwer, Wilna
dc.contributor.authorJoone, Gisela Käthe
dc.contributor.authorJansen van Rensburg, Constance Elizabeth
dc.contributor.authorCronje, Stephanie
dc.contributor.authorRaubenheimer, Helgard G.
dc.date.accessioned2012-05-23T08:31:48Z
dc.date.available2012-05-23T08:31:48Z
dc.date.issued2012-06
dc.description.abstractA series of new neutral mononuclear or dinuclear gold(I) complexes and a cyclic cationic tetranuclear amidogold(I) complex comprising of the phosphines 1,2- bis(dimethylphosphino)ethane (dmpe), μ-1,2–bis(diphenylphosphino)ethane (dppe), μ-1,3- bis(diphenylphosphino)propane (dppp), μ-1,5-bis(diphenylphosphino)pentane (dpppe), μ-1,6- bis(diphenylphosphino)hexane (dpph) or trimethylphosphine, and several N-heterocyclic ring systems (imidazolate, pyrazolate, 1,2,3-triazolate, 1,2,4-triazolate, pyrrolate, 9H-purine-9-ate or 9H-purine-6-amine-9-ate) as ligands, reveal intermolecular aurophilic interactions and 2D channels available for solvent molecules in some of their crystal structures. The antitumour activity of the acyclic gold(I) compounds is highly dependent on the substituents on the phosphorus atoms being highest for phenyl groups and lower for methyl groups. The activity of these compounds against selected cell lines is linked to the length of the carbon bridge between the two phosphorus atoms being highest with a bridge consisting of 5 or 6 carbons. Two compounds with the highest tumour specifities that contain dpppe and pyrazolate (a lipophilic compound) or 1,2,4-triazolate (a hydrophilic compound) induce the apoptic cell death pathway and tolerate a maximum dose of 1.5 μmol/kg when administered to Balb/C mice.en_US
dc.description.sponsorshipClaude Harris Leon Foundation (UEIH), Alexander von Humboldt Stiftung (HGR and SC), NRF (National Research Foundation, South Africa), Harmony Gold Mining Co. Ltd.through Project Autek and the Research Foundation Flanders – FWO (LD)en_US
dc.description.urihttp:// www.sciencedirect.com/science/journal/01620134en_US
dc.identifier.citationUlrike E.I. Horvath, Liliana Dobrzańska, Christoph E. Strasser, Wilna Bouwer, Gisela Joone, Constance E. Jansen van Rensburg, Stephanie Cronje & Helgard G. Raubenheimer, Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity, Journal of Inorganic Biochemistry, vol. 111, no. 6, pp. 80-90 (2012), doi: 10.1016/j.jinorgbio.2012.02.026en_US
dc.identifier.issn0162-0134 (print)
dc.identifier.issn1872-3344 (online)
dc.identifier.other10.1016/j.jinorgbio.2012.02.026
dc.identifier.urihttp://hdl.handle.net/2263/18841
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.rights© 2012 Elsevier Inc. All rights reserved.en_US
dc.subjectAzolateen_US
dc.subjectPurine-ateen_US
dc.subjectGold(I) diphosphinesen_US
dc.subjectCytotoxicityen_US
dc.subjectPyrazolateen_US
dc.subjectAnti-tumouren_US
dc.titleAmides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activityen_US
dc.typePostprint Articleen_US

Files

Original bundle

Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
Horvath_Amides(2012).pdf
Size:
1.51 MB
Format:
Adobe Portable Document Format
Description:
Postprint Article

License bundle

Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
license.txt
Size:
1.71 KB
Format:
Item-specific license agreed upon to submission
Description: