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The reactions of potassium bis(oxalato)platinate dihydrate with two molar equivalents of the potent adenine-based cyclin-dependent kinase inhibitor 2-(1-ethyl-2-hydroxyethylamino )-N6-(benzyl)-9-isopropyladenine (Roscovitine; Ros) and its benzyl-substituted analogues, i.e. 2-(1-ethyl-2-hydroxyethylamino)-N6-(2-methoxybenzyl)-9-isopropyladenine (20MeRos), 2-(1-ethyl-2-hydroxyethylamino)-N6-(3-methoxybenzyl)-9-iso-propyladenine (30MeRos) and 2-(1-ethyl-2-hydroxyethylamino)-N6-(4-methoxybenzyl)-9-isopropyladenine (40MeRos), were performed and the [Pt(ox)(Ros)2]·3/4 H2O (1), [Pt(ox)(2OMeRos)2]·H2O (2), [Pt(ox)(30MeR-os)2] 1/2H2O (3) and [Pt(ox)(4OMeRos)2]·3/4 H2O (4) platinum(II) oxalato complexes were obtained. The methods of the elemental analysis, IR, Raman and NMR spectroscopy, ESI + mass spectrometry, molar conductivity measurement and TG/DTA thermal analysis were performed to characterize the obtained products. The complexes 1—4 involve tetracoordinated central Pt(II) atom with one bidentate-coordinated oxalate dianion (ox) and two monodentate adenine-based molecules (nRos), thus giving the square-planar geometry around the metal centre with a PtN2O2 donor set In vitro cytotoxic activity of the complexes against ovarian carcinoma (A2780), cisplatin resistant ovarian carcinoma (A2780cis), malignant melanoma (G-361), lung carcinoma (A549), cervix epitheloid carcinoma (HeLa), breast adenocarcinoma (MCF7) and osteosarcoma (HOS) human cancer cell lines was evaluated. All the tested complexes exceeded the in vitro cytotoxicity of cisplaan and oxaliplatin against HeLa, A2780cis and, except for 2, also against HOS cancer cells. The complex 1 was also tested for its cytotoxicity in primary cultures of human hepatocytes and it was not found to be hepatotoxic up to the concentration of 50.0 μM.

Titel:	Roscovitine-based CDK inhibitors acting as N-donor ligands in the platinum(II) oxalato complexes: Preparation, characterization and in vitro cytotoxicity
Autor/in / Beteiligte Person:	TRAVNICEK, Zdeněk ; STARHA, Pavel ; POPA, Igor ; VRZAL, Radim ; DVORAK, Zdeněk
Link:	E-Journal im Bestand der UB Hagen? View record from PASCAL Archive
Zeitschrift:	European journal of medicinal chemistry, Jg. 45 (2010), Heft 10, S. 4609-4614
Veröffentlichung:	Kidlington: Elsevier, 2010
Medientyp:	academicJournal
Umfang:	print, 20 ref
ISSN:	0223-5234 (print)
Schlagwort:	Organic chemistry Chimie organique Pharmacology drugs Pharmacologie, galénique Sciences biologiques et medicales Biological and medical sciences Sciences medicales Medical sciences Pharmacologie. Traitements medicamenteux Pharmacology. Drug treatments Anticancéreux Antineoplastic agents Généralités General aspects Enzyme Enzima Métal divalent Complexe Divalent metal Complexes Metal divalente Complejo Métal transition Complexe Transition metal Complexes Metal transición Complejo Antineoplastic agent Anticanceroso Carboxylate Carboxilato Cellule tumorale Tumor cell Célula tumoral Coordinat organique Organic ligand Ligando orgánico Cytotoxicité Cytotoxicity Citotoxicidad Dérivé de la purine Purine derivatives Purina derivado Dérivé du benzène Benzene derivatives Benceno derivado Foie Liver Hígado Homme Human Hombre Hydrate Hydrates Hidrato Hépatocyte Hepatocyte Hepatocito In vitro Inhibiteur des kinases dépendantes des cyclines Cyclin dependent kinase inhibitor Inhibidor cyclin dependent kinase Inhibiteur enzyme Enzyme inhibitor Inhibidor enzima Lignée cellulaire Cell line Línea celular Oxalate Oxalato Platine II Complexe Platinum II Complexes Platino II Complejo Relation structure activité Structure activity relation Relación estructura actividad Spectrométrie RMN NMR spectrometry Espectrometría RMN Substitution coordinat Ligand substitution Sustitución ligando Synthèse chimique Chemical synthesis Síntesis química Toxicité Toxicity Toxicidad Transferases Cyclin-dependent kinase Roscovitine dérivé CDK inhibitors Multinuclear NMR Platinum(II) complexes
Sonstiges:	Nachgewiesen in: PASCAL Archive Sprachen: English Original Material: INIST-CNRS Document Type: Article File Description: text Language: English Author Affiliations: Department of Inorganic Chemistry, Faculty of Science, Palacký University, Tr. 17. listopadu 12, 771 46 Olomouc, Czech Republic ; Deparhnent of Cell Biology and Genetics, Faculty of Science, Palacký University, Šlechtitelü 11, 783 71 Olomouc, Czech Republic Rights: Copyright 2015 INIST-CNRS ; CC BY 4.0 ; Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS Notes: Pharmacological treatments

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Roscovitine-based CDK inhibitors acting as N-donor ligands in the platinum(II) oxalato complexes: Preparation, characterization and in vitro cytotoxicity