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Highly Cytotoxic Molybdenocenes with Strong Metabolic Effects Inhibit Tumour Growth in Mice

A series of six highly lipophilic Cp‐substituted molybdenocenes bearing different bioactive chelating ligands was synthesized and characterized by NMR spectroscopy, mass spectrometry and X‐ray crystallography. In vitro experiments showed a greatly increased cytotoxic potency when compared to the non...

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Detalles Bibliográficos
Autores principales: Fuchs, Valentin, Cseh, Klaudia, Hejl, Michaela, Vician, Petra, Neuditschko, Benjamin, Meier‐Menches, Samuel M., Janker, Lukas, Bileck, Andrea, Gajic, Natalie, Kronberger, Julia, Schaier, Martin, Neumayer, Sophie, Köllensperger, Gunda, Gerner, Christopher, Berger, Walter, Jakupec, Michael A., Malarek, Michael S., Keppler, Bernhard K.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10099754/
https://www.ncbi.nlm.nih.gov/pubmed/36222279
http://dx.doi.org/10.1002/chem.202202648
Descripción
Sumario:A series of six highly lipophilic Cp‐substituted molybdenocenes bearing different bioactive chelating ligands was synthesized and characterized by NMR spectroscopy, mass spectrometry and X‐ray crystallography. In vitro experiments showed a greatly increased cytotoxic potency when compared to the non‐Cp‐substituted counterparts. In vivo experiments performed with the dichlorido precursor, (Ph(2)C−Cp)(2)MoCl(2) and the in vitro most active complex, containing the thioflavone ligand, showed an inhibition of tumour growth. Proteomic studies on the same two compounds demonstrated a significant regulation of tubulin‐associated and mitochondrial inner membrane proteins for both compounds and a strong metabolic effect of the thioflavone containing complex.