Schur, Julia, Luening, Anna, Klein, Axel ORCID: 0000-0003-0093-9619, Koester, Reinhard W. and Ott, Ingo (2019). Platinum alkynyl complexes: Cellular uptake, inhibition of thioredoxin reductase and toxicity in zebrafish embryos. Inorg. Chim. Acta, 495. LAUSANNE: ELSEVIER SCIENCE SA. ISSN 1873-3255

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Abstract

Cytotoxic platinum(II) alkynyl complexes of the type [(COD)Pt(Me)(C CR)] and [(COD)Pt(C CR)2] were evaluated for their cellular uptake, thioredoxin reductase (TrxR) inhibition and toxicity against zebrafish embryos. Quantification of the cellular uptake confirmed lower accumulation levels for the mono-alkynyl derivatives [(COD)Pt(Me)(C CR)] in comparison to the bis-alkynyl complexes [(COD)Pt(C CR)(2)]. Importantly, the complexes were efficient inhibitors of TrxR in contrast to cisplatin, which was not active. Toxicity studies in zebrafish showed lower activity if compared with the cytotoxicity against tumor cells indicating a suitable therapeutic index for the complexes.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Schur, JuliaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Luening, AnnaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Klein, AxelUNSPECIFIEDorcid.org/0000-0003-0093-9619UNSPECIFIED
Koester, Reinhard W.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Ott, IngoUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
URN: urn:nbn:de:hbz:38-143504
DOI: 10.1016/j.ica.2019.118982
Journal or Publication Title: Inorg. Chim. Acta
Volume: 495
Date: 2019
Publisher: ELSEVIER SCIENCE SA
Place of Publication: LAUSANNE
ISSN: 1873-3255
Language: English
Faculty: Faculty of Mathematics and Natural Sciences
Divisions: Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Inorganic Chemistry
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
HETEROCYCLIC CARBENE COMPLEXES; IN-VIVO; BIOLOGICAL-ACTIVITY; ANTICANCER; LIGANDS; DNA; CYTOTOXICITY; BEARING; CELLS; VITROMultiple languages
Chemistry, Inorganic & NuclearMultiple languages
Refereed: Yes
URI: http://kups.ub.uni-koeln.de/id/eprint/14350

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