Functionalization of Ruthenium(II)(η6 -p-cymene)(3-hydroxy-2-pyridone) Complexes with (Thio)Morpholine: Synthesis and Bioanalytical Studies.
Chempluschem
; 82(6): 841-847, 2017 Jun.
Article
em En
| MEDLINE
| ID: mdl-31961568
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 48â
h in aqueous solution, as observed by 1 Hâ
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 kinaseâ
2 (CDK2)/cyclinâ
A kinase inhibitory studies revealed promising activity similar to that of structurally related organometallic compounds.
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Base de dados:
MEDLINE
Idioma:
En
Revista:
Chempluschem
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Nova Zelândia