Publications related to Synthesis of cyclo-β-tripeptides and their biological in vitro evaluation as antiproliferatives against the growth of human cancer cell lines

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

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

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

Kay Severin, Alexey Nazarov, Michael Groessl

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

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

A Novel Cytotoxic Cerium Complex: Aquatrichloridobis(1,10-phenanthroline)cerium(III) (KP776). Synthesis, Characterization, Behavior in H2O, Binding towards Biomolecules, and Antiproliferative Activity

Michael Groessl

The lanthanide complex aquatrichloridobis(1,10-phenanthroline)cerium(III) [Ce(phen)(2)(H2O)Cl-3] (KP776) was fully characterized by elemental analysis, IR-, and H-1- and C-13-NMR spectroscopy, as well as TG/DTA measurements, and its behavior in H2O, import ...

2009

Overcoming multidrug resistance of small-molecule therapeutics through conjugation with releasable octaarginine transporters

Many cancer therapeutic agents elicit resistance that renders them ineffective and often produces cross-resistance to other drugs. One of the most common mechanisms of resistance involves P-glycoprotein (Pgp)-mediated drug efflux. To address this problem, ...

National Academy of Sciences2008

Spongistatins : biological activity and synthetic studies

Pierre Vogel, Sandrine Gerber

During the last two decades, marine organisms such as sponges, tunicates, softcoral and starfish proved to be productive sources of structurally complex metabolites presenting unprecedented architectures.[1] These marine natural products often display unex ...

2008

Development of new anticancer agents based on [alpha]-mannosidase inhibition

Hélène Fiaux

Enzymes that are involved in the synthesis and processing of oligosaccharides, such as glycosidases, are important catalysts for the specific assembly of oligosaccharide structures on proteins. Design and preparation of selective inhibitors of these enzyme ...

EPFL2007

A Polyoxyethylene-Substituted Bimetallic Europium Helicate for Luminescent Staining of Living Cells

Jean-Claude Bünzli, Anne-Sophie Chauvin, Caroline Vandevyver, Bo Song, Steve Comby

The homoditopic ligand

H_2L^{C3}

has been designed to form neutral triple-stranded bimetallic helicates of overall composition [

Ln_2(L^{C3})_3

]. The grafting of the polyoxyethylene fragments ensures water solubility and also favors cell penetration whi ...

2007

Glycosylation pathways as drug targets for cancer: glycosidase inhibitors

Sandrine Gerber

The combined and ordered sequential action of glycosidases and glycosyltransferases in mammalian cell compartments leads to the addition of defined glycans to proteins and lipids. Altered glycosylation patterns, neoexpression, underexpression or overexpres ...

2006

Pyrrolidine derivatives as new inhibitors of alpha-mannosidases and growth inhibitors of human cancer cells

Pierre Vogel, Sandrine Gerber, Hélène Fiaux

New pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L(+)-phenylglycinol and tested for their ability to inhibit 25 commercial glycosidases. The influence of the substitution of the lateral side chain and of the pyrrolidine ring on the enzyme ...

2006

Synthesis of cyclo-β-tripeptides and their biological in vitro evaluation as antiproliferatives against the growth of human cancer cell lines

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

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

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

A Novel Cytotoxic Cerium Complex: Aquatrichloridobis(1,10-phenanthroline)cerium(III) (KP776). Synthesis, Characterization, Behavior in H2O, Binding towards Biomolecules, and Antiproliferative Activity

Overcoming multidrug resistance of small-molecule therapeutics through conjugation with releasable octaarginine transporters

Spongistatins : biological activity and synthetic studies

Development of new anticancer agents based on [alpha]-mannosidase inhibition

A Polyoxyethylene-Substituted Bimetallic Europium Helicate for Luminescent Staining of Living Cells

Glycosylation pathways as drug targets for cancer: glycosidase inhibitors

Pyrrolidine derivatives as new inhibitors of alpha-mannosidases and growth inhibitors of human cancer cells

Overcoming multidrug resistance of small-molecule therapeutics through conjugation with releasable octaarginine transporters

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

Development of new anticancer agents based on [alpha]-mannosidase inhibition

Spongistatins : biological activity and synthetic studies

Glycosylation pathways as drug targets for cancer: glycosidase inhibitors

A Novel Cytotoxic Cerium Complex: Aquatrichloridobis(1,10-phenanthroline)cerium(III) (KP776). Synthesis, Characterization, Behavior in H2O, Binding towards Biomolecules, and Antiproliferative Activity

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

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

A Polyoxyethylene-Substituted Bimetallic Europium Helicate for Luminescent Staining of Living Cells

Pyrrolidine derivatives as new inhibitors of alpha-mannosidases and growth inhibitors of human cancer cells