Functionalization of Ruthenium(II)(η 6 - p -cymene)(3-hydroxy-2-pyridone) Complexes with (Thio)Morpholine: Synthesis and Bioanalytical Studies

Show simple item record Hanif, Muhammad en Meier, SM en Adhireksan, Z en Henke, H en Martic, S en Movassaghi, S en Labib, M en Kandioller, W en Jamieson, Stephen en Hejl, M en Jakupec, MA en Kraatz, H-B en Davey, CA en Keppler, BK en Hartinger, Christian en 2017-07-12T00:32:10Z en 2017-06 en
dc.identifier.citation ChemPlusChem 82(6):841-847 Jun 2017 en
dc.identifier.issn 2192-6506 en
dc.identifier.uri en
dc.description.abstract Hydroxypyr(id)ones constitute an emerging platform for the design of drug molecules, owing to their favorable biocompatibility and toxicity profiles. Herein, [RuII(η6-p-cymene)] complexes with 3-hydroxy-2-pyridinone functionalized with morpholine and thiomorpholine, as a means often used in medicinal chemistry to alter the physicochemical properties of drug compounds, are reported. The compounds underwent hydrolysis of the Ru−Cl bond and the aqua species were stable for up to 48 h in aqueous solution, as observed by 1H NMR spectroscopy and ESI-MS. The compounds formed adducts with amino acids and proteins through cleavage of the pyridinone ligand. Binding experiments to the nucleosome core particle by means of X-ray crystallography revealed similar reactivity and exclusive binding to histidine moieties of the histone proteins. Preliminary cyclin-dependent kinase 2 (CDK2)/cyclin A kinase inhibitory studies revealed promising activity similar to that of structurally related organometallic compounds. en
dc.publisher Wiley-VCH Verlag en
dc.relation.ispartofseries ChemPlusChem en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. en
dc.rights.uri en
dc.title Functionalization of Ruthenium(II)(η 6 - p -cymene)(3-hydroxy-2-pyridone) Complexes with (Thio)Morpholine: Synthesis and Bioanalytical Studies en
dc.type Journal Article en
dc.identifier.doi 10.1002/cplu.201700050 en
pubs.issue 6 en
pubs.begin-page 841 en
pubs.volume 82 en
dc.rights.holder Copyright: Wiley-VCH Verlag en
pubs.end-page 847 en
pubs.publication-status Published en
dc.rights.accessrights en
pubs.subtype Article en
pubs.elements-id 618902 en Medical and Health Sciences en Medical Sciences en Pharmacology en Science en Chemistry en Science Research en Maurice Wilkins Centre (2010-2014) en
dc.identifier.eissn 2192-6506 en
pubs.record-created-at-source-date 2017-07-12 en
pubs.dimensions-id 31961568 en

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