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Alexey Nazarov

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Related publications (37)

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Understanding the interactions of diruthenium anticancer agents with amino acids

Paul Joseph Dyson, Alexey Nazarov, Christian Hartinger

The dinuclear anticancer agents 1,n-bis{chlorido3-(oxo-kappa O)-2-methyl-4-(1H)-pyridinonato-kappa O4-ruthenium(II)}alkane (PyRu2n) exhibit high antiproliferative activity in human cancer cell. Reactivity studies with DNA and protein rev ...

SPRINGER2018

DNA Reactivity Profile of trans-Platinum Planar Amine Derivatives

Alexey Nazarov

New trans-platinum planar amines (TPAs) represent a family of platinum-based drugs with cytotoxicity equivalent to that of cisplatin, but with negligible cross-resistance. According to the substitution pattern around the metal center, distinct DNA adducts ...

2011

{(1R,2R,4R)-4-Methyl-1,2-cyclohexanediamine}oxalatoplatinum(II): A Novel Enantiomerically Pure Oxaliplatin Derivative Showing Improved Anticancer Activity in Vivo

Christian Hartinger, Alexey Nazarov

Novel derivatives of the clinically established anticancer drug oxaliplatin were synthesized. Cytotoxicity of the compounds was studied in six human cancer cell lines by means of the MTT assay. Additionally, most promising complexes were also investigated ...

2010

In vitro anticancer activity and biologically relevant metabolization of organometallic ruthenium complexes with carbohydrate-based ligands

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Olivier Pierre Zava, Michael Groessl, Frédéric Schmitt

The synthesis and in vitro anticancer activity of dihalo(η6-p-cymene)(3,5,6-bicyclophosphite-α-D-glucofuranoside)ruthenium(II) complexes are described. The compds. were characterized by NMR spectroscopy and ESI mass spectrometry, and the mol. structures of ...

2008

Carbohydrate-metal complexes and their potential as anticancer agents

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov

A review. Platinum complex-based chemotherapy is one of the major treatment options of many malignancies. Although severe side effects occur, and only a limited spectrum of tumors can be cured, Pt compds. are used in every second therapy scheme. Thus, many ...

2008

New highly cytotoxic organic and organometallic bexarotene derivatives

Paul Joseph Dyson, Alexey Nazarov, Mathurin Baquié

A series of bifunctional ruthenium(II) arene compounds modified with bexarotene, a retinoid that selectively activates retinoid X receptors inducing cell differentiation and apoptosis and preventing drug resistance, are described. The bexarotene is tethere ...

Elsevier2017

Rational Design of Highly Cytotoxic η6-Arene β-Diketiminato-Ruthenium Complexes

Paul Joseph Dyson, Rosario Scopelliti, Alexey Nazarov, Olivier Pierre Zava, Andrew Douglas Phillips

A series of ruthenium-benzene complexes with β-diketiminate ligands modified with electron-withdrawing groups were prepd. and characterized by NMR spectroscopy, mass spectrometry, and single-crystal x-ray diffraction. The complexes are stable in air and un ...

American Chemical Society2010

Opening the lid on piano-stool complexes: An account of ruthenium(II)-arene complexes with medicinal applications

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov

Interest in the medicinal properties of ruthenium(II)-arene compounds has grown rapidly over the last decade. In this account we describe the origins of the field and subsequently highlight developments in the field, including the design of compounds that ...

Elsevier Science Sa2014

Transferring the Concept of Multinuclearity to Ruthenium Complexes for Improvement of Anticancer Activity

Kay Severin, Alexey Nazarov, Michael Groessl, Christian Hartinger

Multinuclear platinum anticancer complexes are a proven option to overcome resistance of established anticancer compounds. Transferring this concept to ruthenium complexes led to the synthesis of dinuclear Ru(II)-arene compounds containing a bis(pyridinone ...

2009

Maltol-Derived Ruthenium-Cymene Complexes with Tumor Inhibiting Properties: The Impact of Ligand-Metal Bond Stability on Anticancer Activity In Vitro

Christian Hartinger, Alexey Nazarov

Organometallic rutheniumarene compounds bearing a maltol ligand have been shown to be nearly inactive in in vitro anticancer assays, presumably due to the formation of dimeric Ru-II species in aqueous solutions. In an attempt to stabilize such complexes, [ ...

2009

Organometallic antitumour agents with alternative modes of action

Paul Joseph Dyson, Christian Hartinger, Angela Casini, Alexey Nazarov

The therapeutic index of drugs that target DNA, a ubiquitous target present in nearly all cells, is low. Nevertheless, DNA has remained the primary target for medicinal chemists developing metal-based anticancer drugs, although DNA has been essentially aba ...

2010

Influence of the Arene Ligand, the Number and Type of Metal Centers, and the Leaving Group on the in Vitro Antitumor Activity of Polynuclear Organometallic Compounds

Kay Severin, Alexey Nazarov, Christian Hartinger

Dinuclear ruthenium complexes were shown to exhibit strong antiproliferative properties in human tumor cell lines. In order to extend the structure−activity relationships (SARs), a series of new RuII(arene)X complexes (X = Cl, Br, I) linked by pyridinone-b ...

2009

Influence of Structural Variation on the Anticancer Activity of RAPTA-Type Complexes: ptn versus pta

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Anna Katherine Renfrew, Andrew Douglas Phillips

[M(η6-arene)(ptn)Cl]X (M = Ru, Os; arene = p-cymene, benzene, toluene, hexamethylbenzene; ptn = 3,7-dimethyl-7-phospha-1,3,5-triazabicyclo[3.3.1]nonane; X = Cl-, BF4-) were prepd. and characterized spectroscopically. X-ray diffraction was addnl. used to ch ...

2009

Synthesis of [Ru-II(eta(6)-p-cymene)(PPh3)(L)Cl]PF6 complexes with carbohydrate-derived phosphites, imidazole or indazole co-ligands

Christian Hartinger, Alexey Nazarov

Ru-II(arene) complexes of the general formula [Ru-II(eta(6)-p-cymene)(PPh3)(L)Cl]PF6 with L = P- or N-donor systems have been synthesized and characterized. Carbohydrate-derived phosphites, imidazole or indazole have been chosen as co-ligands and different ...

Elsevier2012

Specific DNA structural attributes modulate platinum anticancer drug site selection and cross-link generation

Paul Joseph Dyson, Alexey Nazarov

Heavy metal compounds have toxic and medicinal potential through capacity to form strong specific bonds with macromolecules, and the interaction of platinum drugs at the major groove nitrogen atom of guanine bases primarily underlies their therapeutic acti ...

Oxford University Press2011

Polynuclear Ruthenium, Osmium and Gold Complexes. The Quest for Innovative Anticancer Chemotherapeutics

Christian Hartinger, Alexey Nazarov, Andrew Douglas Phillips

Polynuclear compounds are a relatively new and successful approach in metal-based cancer chemotherapy as typified by the trinuclear Pt compound BBR3464 which was evaluated in clinical trials. In this review, we discuss newer developments of polynuclear rut ...

2011

Synthesis and characterization of a new class of anti-angiogenic agent based on ruthenium clusters

Paul Joseph Dyson, Hubert van den Bergh, Patrycja Nowak-Sliwinska, Alexey Nazarov, Olivier Pierre Zava, Michael Groessl, Mathurin Baquié

New triruthenium-carbonyl clusters derivatized with glucose-modified bicyclophosphite ligands have been synthesized. These compounds were found to have cytostatic and cytotoxic activity and depending on the number of bicyclophosphite ligands, and could be ...

Nature Publishing Group2013

Ligand substitutions between ruthenium-cymene compounds can control protein versus DNA targeting and anticancer activity

Paul Joseph Dyson, Ursula Röthlisberger, Wee Han Ang, Alexey Nazarov, Pablo Campomanes Ramos, Catherine Marie Amélie Clavel, Michael Groessl

Ruthenium compounds have become promising alternatives to platinum drugs by displaying specific activities against different cancers and favourable toxicity and clearance properties. Nonetheless, their molecular targeting and mechanism of action are poorly ...

Nature Research2014

Anthracene-Tethered Ruthenium(II) Arene Complexes as Tools To Visualize the Cellular Localization of Putative Organometallic Anticancer Compounds

Paul Joseph Dyson, Rosario Scopelliti, Christian Hartinger, Wee Han Ang, Alexey Nazarov, Olivier Pierre Zava, Michael Groessl, Albert Ruggi, Frédéric Schmitt, Julie Risse

Anthracene derivatives of ruthenium(II) arene compounds with 1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane (pta) or a sugar phosphite ligand, viz., 3,5,6-bicyclophosphite1,2-O-isopropylidene-alpha-D-glucofuranoside, were prepared in order to evaluate their ...

2012

Tuning the anticancer activity of maltol-derived ruthenium complexes by derivatization of the 3-hydroxy-4-pyrone moiety

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov

Aldol reaction of allomaltol with arom. aldehydes, e.g., RC6H4CHO, R = H, 4-NO2, 4-F, 2-F and 3,4,5-(MeO)3C5H2CHO, gave 2-(hydroxyphenylmethyl)-3-hydroxy-6-methylpyran-4(1)-ones, maltol-derived ligands. Organometallic Ru(II)-arene complexes, [RuCl2(cymene) ...

2009