Publications de Angela Casini | EPFL Graph Search

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A novel ruthenium(II) compound, trans-cis-cis-[Ru(II)Cl-2(DMSO)(2)(2-amino-5-methyl-thiazole)(2)], (I), PMRu52 hereafter, that may be obtained from the previously described (cis and trans)[Ru(II)Cl-2(DMSO)(4)] complexes, was designed, synthesized and chara ...

The antiproliferative properties of a group of 13 structurally diverse gold(III) compounds, including six mononuclear gold(III) complexes, five dinuclear oxo-bridged gold(III) complexes, and two organogold(III) compounds, toward several human tumor cell li ...

The thioredoxin system plays a key role in regulating the overall intracellular redox balance. It basically comprises the small redox protein thioredoxin (Trx), nicotinamide adenine dinucleotide phosphate, in its reduced form (NADPH), and thioredoxin reduc ...

Electrospray ionisation mass spectrometry was used to analyze the reactions of metal compds. with mixts. of selected proteins. Three representative medicinally relevant compds., cisplatin, transplatin and the organometallic ruthenium compd. RAPTA-C, were r ...

More than 99% of currently approved clinical drugs are organic compounds. In contrast, the percentage of metal-containing drugs (metallodrugs) is very low. In cancer chemotherapy, however, platinum coordination compounds represented by cisplatin and deriva ...

The protein binding of anticancer metallodrugs is regarded as an important part in their mode of action both for delivering the active moiety into the tumor but also being responsible for deactivation and/or unwanted side effects. Characterization of prote ...

A series of organometallic compds. of general formula [(arene)M(PTA)nXm]Y (arene = η6-C10H14, η-C5Me5); (M = Ru(II), Os(II), Rh(III) and Ir(III); X = Cl, mPTA; Y = OTf, PF6) have been screened for their cytotoxicity and ability to inhibit cathepsin B in vi ...

Nowadays, gold compounds constitute a family of very promising experimental agents for cancer treatment. Indeed, several gold(I) and gold(III) compounds were shown to manifest outstanding antiproliferative properties in vitro against selected human tumor c ...

Square planar gold(iii) complexes that contain functionalised bipyridine ligands of general formula [Au(NN)Cl2][PF6] [where NN = 2,2'-bipyridine, 4,4'-dimethyl-2,2'-bipyridine, 4,4'-dimethoxy-2,2'-bipyridine and 4,4'-diamino-2,2'-bipyridine] have been prep ...

A method based on the coupling of high resolution size-exclusion liquid chromatography using a polymer stationary phase with inductively coupled plasma mass spectrometry was developed to study the interactions of two metallodrugs - cisplatin and RAPTA-T - ...

Following our strategy of coupling cyclin-dependent kinase (Cdk) inhibitors with organometallic moieties to improve their physicochemical properties and bioavailability, five organoruthenium complexes (1c-5c) of the general formula [RuCl(eta(6)-arene)(L)]C ...

Nowadays, gold compounds occupy a relevant position constituting a promising class of experimental anticancer metallodrugs. Several research efforts have been devoted to the investigations of the pharmacological properties of gold(I) complexes bearing phos ...

Formation of amyloid-beta (A beta)(1-42) amyloid fibrils, a characteristic feature of Alzheimer's disease (AD), was monitored in situ through atomic force microscopy (AFM). Well-structured amyloid fibrils slowly formed in solution within 24 hours for which ...

A novel trans-platinum(II) complex bearing one dimethylamine (dma) and one methylamine (ma) ligand, namely trans-[PtCl2(dma)(ma)], recently synthesised and characterised in our laboratory, displayed relevant antiproliferative properties in vitro, being mor ...

A series of mono-, di-, and trinuclear organometallic alkynyl phosphane gold(I) complexes contg. the stable and water-sol. PTA and DAPTA ligands have been synthesized and characterized. The solid-state structure of one of these compds. was also established ...

The reaction of the five- or six-membered C,N or C,S-palladacycles [(L)PdCl]2 with PTA (1,3,5-triaza-7-phosphaadamantane) led to the monomeric complexes [(L)Pd(PTA)Cl] 6a, 6b and 7 where LH= N,N-dimethyl-1-phenylmethanamine, benzyl(methyl)sulfane or 1-meth ...

Gold metallodrugs form a class of promising antiproliferative agents showing a high propensity to react with proteins. We exploit here X-ray absorption spectroscopy (XAS) methods [both X-ray absorption near-edge spectroscopy (XANES) and extended X-ray abso ...

The synthesis, DNA binding properties and cytotoxicity of a series of Ru(II)-arene complexes containing oligocationic ammonium-functionalized triarylphosphines, of the type Ru(p-cymene)Cl-2(L) (L - oligocationic phosphine), are reported. The complexes are ...

Gold(III) compds. constitute an emerging class of biol. active substances, of special interest as potential anticancer agents. During the past decade a no. of structurally diverse gold(III) complexes were reported to be acceptably stable under physiol.-lik ...

Angela Casini

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Trans-cis-cis-[RuCl2(DMSO)(2)(2-amino-5-methyl-thiazole)(2)], (PMRu52), a novel ruthenium(II) compound acting as a strong inhibitor of cathepsin B

Chemistry, antiproliferative properties, tumor selectivity, and molecular mechanisms of novel gold(III) compounds for cancer treatment: a systematic study

Thioredoxin reductase: A target for gold compounds acting as potential anticancer drugs

Exploring metallodrug-protein interactions by mass spectrometry: comparisons between platinum coordination complexes and an organometallic ruthenium compound

Next-Generation Anticancer Metallodrugs

Mass spectrometric analysis of ubiquitin-platinum interactions of leading anticancer drugs: MALDI versus ESI

Rationalization of the inhibition activity of structurally related organometallic compounds against the drug target cathepsin B by DFT

Molecular Mechanisms and Proposed Targets for Selected Anticancer Gold Compounds

Synthesis, characterisation and biological properties of gold(iii) compounds with modified bipyridine and bipyridylamine ligands

Reactivity of anticancer metallodrugs with serum proteins: New insights from size exclusion chromatography-ICP-MS and ESI-MS

Conjugation of organoruthenium(II) 3-(1H-benzimidzol-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

A new target for gold(I) compounds: glutathione-S.transferase inhibition by auranofin

1) Trace copper(II) or zinc(II) ions drastically modify the aggregation behaviour of Aβ1–42: an AFM study

Solution Behaviour and Biomolecular Interactions of Two Cytotoxic trans-Platinum(II) Complexes Bearing Aliphatic Amine Ligands

Antiproliferative Activity of Gold(I) Alkyne Complexes Containing Water-Soluble Phosphane Ligands

Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

The X-ray Structure of the Adduct between NAMI-A and Carbonic Anhydrase Provides Insights into the Reactivity of this Metallodrug with Proteins

X-ray absorption spectroscopy studies of the adducts formed between cytotoxic gold compounds and two major serum proteins

Ruthenium(II) arene complexes with oligocationic triarylphosphine ligands: Synthesis, DNA interactions and in vitro properties

Gold(III) compounds as anticancer agents: Relevance of gold-protein interactions for their mechanism of action