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Alkynyl gold(I) phosphane complexes: evaluation of structure-activity-relationships for the phosphane ligands, effects on key signaling proteins and preliminary in-vivo studies with a nanoformulated complex

Gold alkynyl complexes with phosphane ligands of the type (alkynyl)Au(I)(phosphane) represent a group of bioorganometallics, which has only recently been evaluated biologically in more detail. Structure-activity-relationship studies regarding the residues of the phosphane ligand (P(Ph)3, P(2-furyl)3...

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Main Authors: Andermark, Vincent (Author) , Göke, Katrin (Author) , Kokoschka, Malte (Author) , Abu El Maaty, Mohamed A. (Author) , Lum, Ching Tung (Author) , Zou, Taotao (Author) , Sun, Raymond Wai-Yin (Author) , Aguiló, Elisabet (Author) , Oehninger, Luciano (Author) , Rodríguez, Laura (Author) , Bunjes, Heike (Author) , Wölfl, Stefan (Author) , Che, Chi-Ming (Author) , Ott, Ingo (Author)
Format: Article (Journal)
Language:English
Published: 2016
In: Journal of inorganic biochemistry
Year: 2015, Volume: 160, Pages: 140-148
ISSN:1873-3344
DOI:10.1016/j.jinorgbio.2015.12.020
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.jinorgbio.2015.12.020
Verlag, lizenzpflichtig, Volltext: http://www.sciencedirect.com/science/article/pii/S0162013415301549
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Author Notes:Vincent Andermark, Katrin Göke, Malte Kokoschka, Mohamed A. Abu el Maaty, Ching Tung Lum, Taotao Zou, Raymond Wai-Yin Sun, Elisabet Aguiló, Luciano Oehninger, Laura Rodríguez, Heike Bunjes, Stefan Wölfl, Chi-Ming Che, Ingo Ott
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Summary:Gold alkynyl complexes with phosphane ligands of the type (alkynyl)Au(I)(phosphane) represent a group of bioorganometallics, which has only recently been evaluated biologically in more detail. Structure-activity-relationship studies regarding the residues of the phosphane ligand (P(Ph)3, P(2-furyl)3, P(DAPTA)3, P(PTA)3, P(Et)3, P(Me)3) of complexes with an 4-ethynylanisole alkyne ligand revealed no strong differences concerning cytotoxicity. However, a relevant preference for the heteroatom free alkyl/aryl residues concerning inhibition of the target enzyme thioredoxin reductase was evident. Complex 1 with the triphenylphosphane ligand was selected for further studies, in which clear effects on cell morphology were monitored by time-lapse microscopy. Effects on cellular signaling were determined by ELISA microarrays and showed a significant induction of the phosphorylation of ERK1 (extracellular signal related kinase 1), ERK2 and HSP27 (heat shock protein 27) in HT-29 cells. Application of 1 in-vivo in a mouse xenograft model was found to be challenging due to the low solubility of the complex and required a formulation strategy based on a peanut oil nanoemulsion.
Item Description:Available online 30 December 2015
Gesehen am 17.08.2020
Physical Description:Online Resource
ISSN:1873-3344
DOI:10.1016/j.jinorgbio.2015.12.020

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