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List of works by Michael A. Jakupec

3-Hydroxyflavones vs. 3-hydroxyquinolinones: structure-activity relationships and stability studies on Ru(II)(arene) anticancer complexes with biologically active ligands

scientific article published on May 2013

A SAR study of novel antiproliferative ruthenium and osmium complexes with quinoxalinone ligands in human cancer cell lines

scientific article

A glucose derivative as natural alternative to the cyclohexane-1,2-diamine ligand in the anticancer drug oxaliplatin?

scientific article

A highly cytotoxic modified paullone ligand bearing a TEMPO free-radical unit and its copper(II) complex as potential hR2 RNR inhibitors

scientific article published on November 2013

A novel class of bis- and tris-chelate diam(m)inebis(dicarboxylato)platinum(IV) complexes as potential anticancer prodrugs.

scientific article

A novel cytotoxic cerium complex: aquatrichloridobis(1,10-phenanthroline)cerium(III) (KP776). Synthesis, characterization, behavior in H2O, binding towards biomolecules, and antiproliferative activity

scientific article

Am(m)ines make the difference: organoruthenium am(m)ine complexes and their chemistry in anticancer drug development

scientific article published on 22 January 2013

An Organoruthenium Anticancer Agent Shows Unexpected Target Selectivity For Plectin.

scientific article published on 26 May 2017

Anticancer activity of methyl-substituted oxaliplatin analogs

scientific article published on 13 February 2012

Anticancer activity of the lanthanum compound [tris(1,10-phenanthroline)lanthanum(III)]trithiocyanate (KP772; FFC24).

scientific article published on 15 December 2005

Antitumor pentamethylcyclopentadienyl rhodium complexes of maltol and allomaltol: synthesis, solution speciation and bioactivity

scientific article published on 3 February 2014

Antitumour metal compounds: more than theme and variations

scientific article

Aqueous chemistry and antiproliferative activity of a pyrone-based phosphoramidate Ru(arene) anticancer agent.

scientific article

Behavior of platinum(iv) complexes in models of tumor hypoxia: cytotoxicity, compound distribution and accumulation

scientific article published on 10 February 2016

Biological activity of ruthenium and osmium arene complexes with modified paullones in human cancer cells.

scientific article

Biological evaluation of novel thiomaltol-based organometallic complexes as topoisomerase IIα inhibitors

scientific article published on 19 March 2020

Biological properties of novel ruthenium- and osmium-nitrosyl complexes with azole heterocycles

scientific article

Bis- and Tetrakis(carboxylato)platinum(IV) complexes with mixed axial ligands - synthesis, characterization, and cytotoxicity

scientific article

Bulky N(,N)-(di)alkylethane-1,2-diamineplatinum(II) compounds as precursors for generating unsymmetrically substituted platinum(IV) complexes.

scientific article published on 21 June 2013

Cellular accumulation and DNA interaction studies of cytotoxic trans-platinum anticancer compounds

scientific article published on 7 January 2012

Comparative equilibrium and structural studies of new pentamethylcyclopentadienyl rhodium complexes bearing (O,N) donor bidentate ligands

Comparative studies of oxaliplatin-based platinum(iv) complexes in different in vitro and in vivo tumor models

scientific article

Complexes of N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid with group 12 metals and vanadium-Synthesis, structure and bioactivity of the vanadium complex

scientific article published on 11 April 2015

Conjugation of organoruthenium(II) 3-(1H-benzimidazol-2-yl)pyrazolo[3,4-b]pyridines and indolo[3,2-d]benzazepines to recombinant human serum albumin: a strategy to enhance cytotoxicity in cancer cells

scientific article published on 23 November 2011

Cytotoxicity and preliminary mode of action studies of novel 2-aryl-4-thiopyrone-based organometallics.

scientific article published on 2 December 2015

Design, synthesis, nuclear localization, and biological activity of a fluorescent duocarmycin analog, HxTfA.

scientific article published on 5 March 2018

Development of an experimental protocol for uptake studies of metal compounds in adherent tumor cells

scientific article

Dicopper(II) and dizinc(II) complexes with nonsymmetric dinucleating ligands based on indolo[3,2-c]quinolines: synthesis, structure, cytotoxicity, and intracellular distribution.

scientific article published on 16 August 2013

Effect of metal ion complexation and chalcogen donor identity on the antiproliferative activity of 2-acetylpyridine N,N-dimethyl(chalcogen)semicarbazones.

scientific article published on 31 July 2007

En route to osmium analogues of KP1019: synthesis, structure, spectroscopic properties and antiproliferative activity of trans-[Os(IV)Cl4(Hazole)2]

scientific article published on 8 July 2011

Fine-Tuning the Activation Mode of an 1,3-Indandione-Based Ruthenium(II)-Cymene Half-Sandwich Complex by Variation of Its Leaving Group

scientific article published on 27 June 2019

From Pyrone to Thiopyrone Ligands−Rendering Maltol-Derived Ruthenium(II)−Arene Complexes That Are Anticancer Active in Vitro

From bench to bedside--preclinical and early clinical development of the anticancer agent indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019 or FFC14A).

scientific article

From hydrolytically labile to hydrolytically stable Ru(II)-arene anticancer complexes with carbohydrate-derived co-ligands.

scientific article published on 14 October 2010

Front Cover: Oxoplatin‐Based Pt(IV) Lipoate Complexes and Their Biological Activity (Chem. Biodiversity 10/2022)

scientific article published in 2022

Gallium in cancer treatment

scientific article published on 01 January 2004

Gallium(III) and iron(III) complexes of alpha-N-heterocyclic thiosemicarbazones: synthesis, characterization, cytotoxicity, and interaction with ribonucleotide reductase.

scientific article published on 22 February 2007

Guanidine platinum(II) complexes: synthesis, in vitro antitumor activity, and DNA interactions.

scientific article published on 22 December 2013

Heterocyclic complexes of ruthenium(III) induce apoptosis in colorectal carcinoma cells.

scientific article published on 16 October 2004

Highly cytotoxic copper(II) complexes with modified paullone ligands

scientific article

Identification of the structural determinants for anticancer activity of a ruthenium arene peptide conjugate

scientific article published on 27 May 2013

Impact of metal coordination on cytotoxicity of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (triapine) and novel insights into terminal dimethylation.

scientific article published in August 2009

Impact of the equatorial coordination sphere on the rate of reduction, lipophilicity and cytotoxic activity of platinum(IV) complexes

scientific article published on 16 June 2017

Improved reaction conditions for the synthesis of new NKP-1339 derivatives and preliminary investigations on their anticancer potential

scientific article

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

scientific article

Influence of ascorbic acid on the activity of the investigational anticancer drug KP1019.

scientific article published on 26 June 2011

Influence of extracellular pH on the cytotoxicity, cellular accumulation, and DNA interaction of novel pH-sensitive 2-aminoalcoholatoplatinum(II) complexes

scientific article published on 26 January 2013

Influence of reducing agents on the cytotoxic activity of platinum(IV) complexes: induction of G2/M arrest, apoptosis and oxidative stress in A2780 and cisplatin resistant A2780cis cell lines.

scientific article published on July 2015

Influence of the Arene Ligand and the Leaving Group on the Anticancer Activity of (Thio)maltol Ruthenium(II)–(η6-Arene) Complexes

Influence of the Arene Ligand, the Number and Type of Metal Centers, and the Leaving Group on thein VitroAntitumor Activity of Polynuclear Organometallic Compounds

Influence of the Spacer Length on thein VitroAnticancer Activity of Dinuclear Ruthenium−Arene Compounds

Influence of the π-coordinated arene on the anticancer activity of ruthenium(II) carbohydrate organometallic complexes

scientific article

Inhibitory Effects of the Ruthenium Complex KP1019 in Models of Mammary Cancer Cell Migration and Invasion.

scientific article published on 17 September 2009

Intrinsic and Acquired Forms of Resistance against the Anticancer Ruthenium Compound KP1019 [Indazolium trans-[tetrachlorobis(1H-indazole)ruthenate (III)] (FFC14A)

scientific article published on 26 August 2004

Introducing N-, P-, and S-donor leaving groups: an investigation of the chemical and biological properties of ruthenium, rhodium and iridium thiopyridone piano stool complexes

scientific article published on 02 November 2020

Introducing the 4-Phenyl-1,2,3-Triazole Moiety as a Versatile Scaffold for the Development of Cytotoxic Ruthenium(II) and Osmium(II) Arene Cyclometalates

scientific article published on 20 December 2016

Is the reactivity of M(II)-arene complexes of 3-hydroxy-2(1H)-pyridones to biomolecules the anticancer activity determining parameter?

scientific article published on September 2010

KP1019, a new redox-active anticancer agent--preclinical development and results of a clinical phase I study in tumor patients

scientific article published on October 2008

L- and D-proline thiosemicarbazone conjugates: coordination behavior in solution and the effect of copper(II) coordination on their antiproliferative activity.

scientific article published on 13 August 2012

LA-ICP-MS imaging in multicellular tumor spheroids - a novel tool in the preclinical development of metal-based anticancer drugs.

scientific article published on 25 January 2016

Maleimide-functionalised organoruthenium anticancer agents and their binding to thiol-containing biomolecules

scientific article published on 14 October 2011

Maltol-derived ruthenium-cymene complexes with tumor inhibiting properties: the impact of ligand-metal bond stability on anticancer activity in vitro

scientific article published on November 2009

Metal-Arene Complexes with Indolo[3,2-c]-quinolines: Effects of Ruthenium vs Osmium and Modifications of the Lactam Unit on Intermolecular Interactions, Anticancer Activity, Cell Cycle, and Cellular Accumulation

scientific article published on 17 January 2013

Metal-based paullones as putative CDK inhibitors for antitumor chemotherapy

scientific article published on 13 November 2007

Molecular mode of action of NKP-1339 - a clinically investigated ruthenium-based drug - involves ER- and ROS-related effects in colon carcinoma cell lines

scientific article published on 18 March 2016

Morpho‐metabotyping the oxidative stress response

scientific article published in 2021

Multi-scale imaging of anticancer platinum(iv) compounds in murine tumor and kidney

scientific article published on 03 February 2016

Multidrug-resistant cancer cells are preferential targets of the new antineoplastic lanthanum compound KP772 (FFC24).

scientific article

N- and S-donor leaving groups in triazole-based ruthena(ii)cycles: potent anticancer activity, selective activation, and mode of action studies

scientific article published on 9 March 2018

NKP-1339, the first ruthenium-based anticancer drug on the edge to clinical application

article by Robert Trondl et al published 4 April 2014 in Chemical Science

NanoSIMS combined with fluorescence microscopy as a tool for subcellular imaging of isotopically labeled platinum-based anticancer drugs

New platinum-oxicam complexes as anti-cancer drugs. Synthesis, characterization, release studies from smart hydrogels, evaluation of reactivity with selected proteins and cytotoxic activity in vitro

scientific article published on 27 March 2010

Novel di- and tetracarboxylatoplatinum(IV) complexes. Synthesis, characterization, cytotoxic activity, and DNA platination.

scientific article published on 22 November 2007

Novel glucose-ferrocenyl derivatives: synthesis and properties

Novel metal(ii) arene 2-pyridinecarbothioamides: a rationale to orally active organometallic anticancer agents

Novel tetracarboxylatoplatinum(IV) complexes as carboplatin prodrugs.

scientific article

Organometallic anticancer complexes of lapachol: metal centre-dependent formation of reactive oxygen species and correlation with cytotoxicity

scientific article published on April 2013

Organometallic indolo[3,2-c]quinolines versus indolo[3,2-d]benzazepines: synthesis, structural and spectroscopic characterization, and biological efficacy

scientific article

Osmium NAMI-A analogues: synthesis, structural and spectroscopic characterization, and antiproliferative properties.

scientific article published on 12 May 2007

Osmium(II)--versus ruthenium(II)--arene carbohydrate-based anticancer compounds: similarities and differences.

scientific article published on 2 July 2010

Osmium(IV) complexes with 1H- and 2H-indazoles: tautomer identity versus spectroscopic properties and antiproliferative activity

scientific article

Pharmacological properties of cerium compounds.

scientific article

Physicochemical Studies and Anticancer Potency of Ruthenium η-p-Cymene Complexes Containing Antibacterial Quinolones

scientific article published on 6 April 2011

Plecstatin-1 induces an immunogenic cell death signature in colorectal tumour spheroids

scientific article published on 09 December 2020

Post-digestion stabilization of osmium enables quantification by ICP-MS in cell culture and tissue

scientific article published on 01 June 2017

Preclinical characterization of anticancer gallium(III) complexes: solubility, stability, lipophilicity and binding to serum proteins

scientific article published on 25 July 2006

Recent developments in the field of tumor-inhibiting metal complexes.

scientific article

Redox behavior of tumor-inhibiting ruthenium(iii) complexes and effects of physiological reductants on their binding to GMP

scientific article published on 11 January 2006

Redox-active antineoplastic ruthenium complexes with indazole: correlation of in vitro potency and reduction potential

scientific article

Resistance against novel anticancer metal compounds: differences and similarities

scientific article published on February 2008

Reversion of Structure-Activity Relationships of Antitumor Platinum Complexes by Acetoxime but Not Hydroxylamine Ligands

scientific article published on 18 October 2006

Rollover Cyclometalated Bipyridine Platinum Complexes as Potent Anticancer Agents: Impact of the Ancillary Ligands on the Mode of Action

scientific article published on 14 February 2018

Ruthenium and Other Non-Platinum Anticancer Compounds

Ruthenium- and osmium-arene complexes of 8-substituted indolo[3,2-c]quinolines: Synthesis, X-ray diffraction structures, spectroscopic properties, and antiproliferative activity ⬇️

scientific article published on December 1, 2012

Ruthenium- and osmium-arene-based paullones bearing a TEMPO free-radical unit as potential anticancer drugs.

scientific article

Ruthenium-nitrosyl complexes with glycine, L-alanine, L-valine, L-proline, D-proline, L-serine, L-threonine, and L-tyrosine: synthesis, X-ray diffraction structures, spectroscopic and electrochemical properties, and antiproliferative activity

scientific article published on 20 February 2014

Ruthenium− and Osmium−Arene Complexes of 2-Substituted Indolo[3,2-c]quinolines: Synthesis, Structure, Spectroscopic Properties, and Antiproliferative Activity ⬇️

scientific article published on December 27, 2010

Single Spheroid Metabolomics: Optimizing Sample Preparation of Three-Dimensional Multicellular Tumor Spheroids

scientific article published on 14 December 2019

Solid-phase synthesis of oxaliplatin-TAT peptide bioconjugates.

scientific article published on 27 January 2012

Striking difference in antiproliferative activity of ruthenium- and osmium-nitrosyl complexes with azole heterocycles

scientific article

Structure-activity relationships for NAMI-A-type complexes (HL)[trans-RuCl4L(S-dmso)ruthenate(III)] (L = imidazole, indazole, 1,2,4-triazole, 4-amino-1,2,4-triazole, and 1-methyl-1,2,4-triazole): aquation, redox properties, protein binding, and anti

scientific article published on 3 April 2007

Structure-activity relationships of highly cytotoxic copper(II) complexes with modified indolo[3,2-c]quinoline ligands.

scientific article published on 27 October 2010

Structure-activity relationships of targeted RuII(η6-p-cymene) anticancer complexes with flavonol-derived ligands

scientific article

Synthesis and characterization of novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes with higher cytotoxicity than cisplatin

scientific article

Synthesis and in vitro antitumor potency of (cyclohexane-1,2-diamine)platinum(II) complexes with aminotris(methylenephosphonic acid) as bone-seeking ligand

scientific article

Synthesis and in vivo anticancer evaluation of poly(organo)phosphazene-based metallodrug conjugates.

scientific article

Synthesis, Modification, and Biological Evaluation of a Library of Novel Water-Soluble Thiopyridone-Based Organometallic Complexes and Their Unexpected (Biological) Behavior

scientific article published on 20 January 2020

Synthesis, X-ray diffraction structures, spectroscopic properties, and in vitro antitumor activity of isomeric (1H-1,2,4-triazole)Ru(III) complexes.

scientific article published on September 2003

Synthesis, characterization, and cytotoxic activity of novel potentially pH-sensitive nonclassical platinum(II) complexes featuring 1,3-dihydroxyacetone oxime ligands.

scientific article published on 27 September 2011

Synthesis, crystal structure and cytotoxicity of new oxaliplatin analogues indicating that improvement of anticancer activity is still possible.

scientific article published on August 2004

Synthesis, crystal structure and pH dependent cytotoxicity of (SP-4-2)-bis(2-aminoethanolato-κ2N,O)platinum(II) – a representative of novel pH sensitive anticancer platinum complexes

Synthesis, structure, spectroscopic and in vitro antitumour studies of a novel gallium(III) complex with 2-acetylpyridine (4)N-dimethylthiosemicarbazone.

scientific article

Synthesis, structure, spectroscopic properties, and antiproliferative activity in vitro of novel osmium(III) complexes with azole heterocycles.

scientific article

Synthesis, structures and in vitro cytotoxicity of some cationic cis-platinum(II) complexes containing chelating thiocarbamates

scientific article published on 31 August 2010

Target profiling of an antimetastatic RAPTA agent by chemical proteomics: relevance to the mode of action

scientific article published on 9 February 2015

Targeting the DNA-topoisomerase complex in a double-strike approach with a topoisomerase inhibiting moiety and covalent DNA binder.

scientific article published on 12 April 2012

Tetra-(p-tolyl)antimony(III)-Containing Heteropolytungstates, [{(p-tolyl)SbIII}4(A-α-XW9O34)2]n- (X = P, As, or Ge): Synthesis, Structure, and Study of Antibacterial and Antitumor Activity

scientific article published on 10 February 2020

Tetracarboxylatoplatinum(IV) complexes featuring monodentate leaving groups - A rational approach toward exploiting the platinum(IV) prodrug strategy

scientific article published on 28 August 2015

The First Anticancer Tris(pyrazolyl)borate Molybdenum(IV) Complexes: Tested in Vitro and in Vivo-A Comparison of O,O-, S,O-, and N,N-Chelate Effects

scientific article published on 19 November 2019

The first metal-based paullone derivative with high antiproliferative activity in vitro.

scientific article published in March 2006

The first ruthenium-based paullones: syntheses, X-ray diffraction structures, and spectroscopic and antiproliferative properties in vitro

scientific article published on 3 April 2007

The gallium complex KP46 exerts strong activity against primary explanted melanoma cells and induces apoptosis in melanoma cell lines

scientific article

The heterocyclic ruthenium(III) complex KP1019 (FFC14A) causes DNA damage and oxidative stress in colorectal tumor cells.

scientific article

The role of the equatorial ligands for the redox behavior, mode of cellular accumulation and cytotoxicity of platinum(IV) prodrugs.

scientific article published on 17 March 2016

Thermodynamic Genome-Scale Metabolic Modeling of Metallodrug Resistance in Colorectal Cancer

scientific article published in 2021

Thiomaltol-Based Organometallic Complexes with 1-Methylimidazole as Leaving Group: Synthesis, Stability, and Biological Behavior.

scientific article published on 19 October 2016

Three-dimensional and co-culture models for preclinical evaluation of metal-based anticancer drugs.

scientific article

Towards targeting anticancer drugs: ruthenium(ii)-arene complexes with biologically active naphthoquinone-derived ligand systems.

scientific article

Transferrin binding and transferrin-mediated cellular uptake of the ruthenium coordination compound KP1019, studied by means of AAS, ESI-MS and CD spectroscopy

article published in 2004

Transferring the concept of multinuclearity to ruthenium complexes for improvement of anticancer activity

scientific article

Triapine and a more potent dimethyl derivative induce endoplasmic reticulum stress in cancer cells.

scientific article published on 30 December 2013

Tumour-inhibiting platinum complexes--state of the art and future perspectives.

scientific article

Tuning of lipophilicity and cytotoxic potency by structural variation of anticancer platinum(IV) complexes

scientific article published on October 2010

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

Unsymmetric mono- and dinuclear platinum(IV) complexes featuring an ethylene glycol moiety: synthesis, characterization, and biological activity

scientific article published on 17 December 2012

Water-soluble cationic derivatives of indirubin, the active anticancer component from Indigo naturalis

scientific article

X-ray absorption near edge structure spectroscopy to resolve the in vivo chemistry of the redox-active indazolium trans-[Tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019).

scientific article published on 31 January 2013

[Os(IV)Cl(5)(Hazole)](-) complexes: synthesis, structure, spectroscopic properties, and antiproliferative activity

scientific article

{(1R,2R,4R)-4-methyl-1,2-cyclohexanediamine}oxalatoplatinum(II): a novel enantiomerically pure oxaliplatin derivative showing improved anticancer activity in vivo

scientific article

{Ru(CO)x}-Core complexes with benzimidazole ligands: synthesis, X-ray structure and evaluation of anticancer activity in vivo.

scientific article published on 16 February 2017

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