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SANDRA LAZZARI
Docente a contratto
Dipartimento di Scienze Chimiche e Geologiche sede ex-Chimica
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Pubblicazioni
- USO DI INIBITORI DELLA PTERIDINA REDUTTASI PER LA PREVENZIONE E/O IL TRATTAMENTO DI INFEZIONI PARASSITARIE
[Brevetto]
Costi, Maria Paola; Wade, R; Henrich, S; D, Montejenues; Ferrari, Stefania; Venturelli, Alberto; Lazzari, Sandra; Guerrieri, Davide; Nerini, Erika
abstract
La presente invenzione riguarda l’uso di composti inibitori dellapteridina reduttasi per la prevenzione e/o il trattamento di infezioni parassitarie.
2017
- Design, synthesis and biological evaluation of non-covalent AmpC Beta-Lactamases inhibitors
[Articolo su rivista]
Genovese, Filippo; Lazzari, Sandra; Venturi, Ettore; Costantino, Luca; Blazquez, Jesus; Ibacache Quiroga, · Claudia; Costi, Maria Paola; Tondi, Donatella
abstract
Bacterial resistance represents a worldwide emergency threatening the efficacy of all available antibiotics. Among the several resistance mechanisms developed by bacteria, beta-lactamases enzymes (BLs), able to inactivate most beta-lactam core antibiotics, represent a key target to block prolonging antibiotics half-life. Several approaches aimed at inhibiting BLs have been so far undertaken, mainly involving beta-lactam like or covalent inhibitors. Applying a structure based de novo design approach, we recently discovered a novel, non-covalent and competitive inhibitor of AmpC beta lactamases: it has a Ki of 1 µM, a ligand efficiency of 0.38 kcal ∙ mol–1 and lead-like physical properties. Moreover, it reverts resistance to ceftazidime in bacterial pathogens expressing AmpC and does not up-regulate beta-lactamase expression in cell culture. Its features make it a good candidate for chemical optimization: starting from its crystallographic complex with AmpC, eleven analogues were designed to complement additional AmpC sites, then synthesized and tested against clinical resistant pathogens. While the new inhibitors maintain similar in vitro activity as the starting lead, some of them exert a higher potency in in vivo tests, showing improved synergic potency with ceftazidime in resistant clinically isolated strains.
2017
- Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To InhibitTrypanosoma bruceiPteridine Reductase in Support of Early-Stage Drug Discovery
[Articolo su rivista]
Linciano, Pasquale; Dawson, Alice; Pöhner, Ina; Costa, David M; Sá, Monica S; Cordeiro-da-Silva, Anabela; Luciani, Rosaria; Gul, Sheraz; Witt, Gesa; Ellinger, Bernhard; Kuzikov, Maria; Gribbon, Philip; Reinshagen, Jeanette; Wolf, Markus; Behrens, Birte; Hannaert, Véronique; Michels, Paul A M; Nerini, Erika; Pozzi, Cecilia; di Pisa, Flavio; Landi, Giacomo; Santarem, Nuno; Ferrari, Stefania; Saxena, Puneet; Lazzari, Sandra; Cannazza, Giuseppe; Freitas-Junior, Lucio H; Moraes, Carolina B; Pascoalino, Bruno S; Alcântara, Laura M; Bertolacini, Claudia P; Fontana, Vanessa; Wittig, Ulrike; Müller, Wolfgang; Wade, Rebecca C; Hunter, William N; Mangani, Stefano; Costantino, Luca; Costi, Maria P
abstract
Pteridine reductase-1 (PTR1) is a promising drug target for the treatment of trypanosomiasis. We investigated the potential of a previously identified class of thiadiazole inhibitors of Leishmania major PTR1 for activity against Trypanosoma brucei (Tb). We solved crystal structures of several TbPTR1-inhibitor complexes to guide the structure-based design of new thiadiazole derivatives. Subsequent synthesis and enzyme-and cell-based assays confirm new, mid-micromolar inhibitors of TbPTR1 with low toxicity. In particular, compound 4m, a biphenyl-thiadiazole-2,5-diamine with IC50 = 16 mu M, was able to potentiate the antitrypanosomal activity of the dihydrofolate reductase inhibitor methotrexate (MTX) with a 4.1-fold decrease of the EC50 value. In addition, the antiparasitic activity of the combination of 4m and MTX was reversed by addition of folic acid. By adopting an efficient hit discovery platform, we demonstrate, using the 2-amino-1,3,4-thiadiazole scaffold, how a promising tool for the development of anti-T. brucei agents can be obtained.
2011
- How glucosylation triggers physical–chemical properties of curcumin: an experimental and theoretical study.
[Articolo su rivista]
Benassi, Rois; Ferrari, Erika; Lazzari, Sandra; Pignedoli, Francesca; F., Spagnolo; Saladini, Monica
abstract
In the present study, we investigate the structures of glucosylated curcumin derivatives with DFT at B3LYP/6-31G*level. A conformational analysis is performed in order to determine the conformational minimum (GS) and rotationaltransition state (TS) of curcumin derivatives and then their electronic features are evaluated. HOMO and LUMOfrontier orbitals and maps of electron density potential (MEPs) are plotted and compared. In order to correlate theirpredicted spectroscopic properties with IR, UV–vis and NMR experimental data we extended the theoretical study onelectronic properties to different solvents (H2O, MeOH, ACN, DMSO). The main finding is that the curcuminic coremaintains the same geometrical and electronic structures in all compounds miming the metal coordination capabilityshowed by curcumin. Therefore, wemay confirm that the presence of glucose does not affect the electronic propertiesof the derivatives.
2011
- Identification of the binding modes of N-phenylphthalimides inhibiting bacterial thymidylate synthase through X-ray crystallography screening.
[Articolo su rivista]
Mangani, S; Cancian, Laura; Leone, R; Pozzi, C; Lazzari, Sandra; Luciani, Rosaria; Ferrari, Stefania; Costi, Maria Paola
abstract
To identify specific bacterial thymidylate synthase (TS) inhibitors, we exploited phenolphthalein (PTH), which inhibits both bacterial and human enzymes. The X-ray crystal structure of Lactobacillus casei TS (LcTS) that binds PTH showed multiple binding modes of the inhibitor, which prevented a classical structure-based drug design approach. To overcome this issue, we synthesized two phthalimidic libraries that were tested against TS enzymes and then we performed X-ray crystallographic screening of the active compounds. Compounds 6A, 8A, and 12A showed 40-fold higher affinity for bacterial TS than human TS. The X-ray crystallographic screening characterized the binding mode of six inhibitors in complexes with LcTS. Of these, 20A, 23A, and 24A showed a common unique binding mode, whereas 8A showed a different, unique binding mode. A comparative analysis of the LcTS X-ray complexes that were obtained with the pathogenic TS enabled the selection of compounds 8A and 23A as specific compounds and starting points to be exploited for the specific inhibition of pathogen enzymes.
2011
- Virtual screening identification of nonfolate compounds, including a CNS drug, as antiparasitic agents inhibiting pteridine reductase
[Articolo su rivista]
Ferrari, Stefania; Morandi, Federica; Motiejunas, D.; Nerini, Erika; Henrich, S.; Luciani, Rosaria; Venturelli, Alberto; Lazzari, Sandra; Calo', Samuele; Gupta, S.; Hannaert, V.; Michels, P. A. M.; Wade, R. C.; Costi, Maria Paola
abstract
Folate analogue inhibitors of Leishmania major pteridine reductase (PTR1) are potential anti-parasitic drug candidates for combined therapy with dihydrofolate reductase (DHFR) inhibitors. To identify new molecules with specificity for PTR1, we carried out a virtual screening of the Available Chemicals Directory (ACD) database to select compounds that could interact with L. major PTR1 but not with human DHFR. Through two rounds of drug discovery, we successfully identified eighteen drug-like molecules with low micromolar affinities and high in vitro specificity profiles. Their efficacy against Leishmania species was studied in cultured cells of the promastigote stage, using the compounds both alone and in combination with 1 (pyrimethamine; 5-(4-Chlorophenyl)-6-ethylpyrimidine-2,4-diamine). Six compounds showed efficacy only in combination. In toxicity tests against human fibroblasts, several compounds showed low toxicity. One compound, 5c (riluzole; 6-(trifluoromethoxy)-1,3-benzothiazol-2-ylamine), a known drug approved for CNS pathologies was active in combination and is suitable for early pre-clinical evaluation of its potential for label extension as a PTR1 inhibitor and anti-parasitic drug candidate.
2010
- Allosteric Inhibition of human Thymidylate Synthase.
[Abstract in Atti di Convegno]
S., Henrich; O., Salo Ahen; D., Garg; Cardinale, Daniela; Ferrari, Stefania; Franchini, Silvia; Genovese, Filippo; Guaitoli, Giambattista; Lazzari, Sandra; Venturelli, Alberto; S., Mangani; Costi, Maria Paola; R. C., Wade
abstract
Thymidylate synthase (TS) takes part in the folate pathway and is a dimeric enzyme that catalyzes the conversion from dUMP to dTMP. This reaction step is essential for all cells, but especially for fast growing cancer cells, making TS an important target for cancer treatment. Most of the clinical drugs for inhibiting TS are substrate or cofactor analogues that give rise to resistance after a certain time. The aim of the LIGHTS EU project is to overcome such resistance to inhibitors by interfering with TS dimerizationusing low molecular weight compounds and peptides binding to allosteric sites.
2010
- Tethering low affinity ligands to the dimeric interface of human thymidylate synthase.
[Relazione in Atti di Convegno]
Costi, Maria Paola; Genovese, Filippo; Franchini, Silvia; Venturelli, Alberto; Lazzari, Sandra; Farina, Davide Salvatore Francesco; Pirondi, Silvia; R. C., Wade; S., Mangani; C., Pozzi; S., Henrich; Ferrari, Stefania; Ponterini, Glauco; Guaitoli, Giambattista; G., Cruciani
abstract
...
2009
- Curcumin derivatives: molecular basis of their anti-cancer activity.
[Articolo su rivista]
Basile, Valentina; Ferrari, Erika; Lazzari, Sandra; Belluti, S.; Pignedoli, Francesca; Imbriano, Carol
abstract
Curcumin, a phenolic compound from the plant Curcuma longa L., has shown a wide-spectrum of chemopreventive, anti-oxidant and anti-tumor properties. Although its promising chemotherapeutic activity, preclinical and clinical studies highlight Curcumin limited therapeutic application due to its instability in physiological conditions. To improve its stability and activity, many derivatives have been synthesized and studied, among which bis-DemethoxyCurcumin (bDMC) and diAcetylCurcumin (DAC). In this report, we show that both bDMC and DAC are more stable than Curcumin in physiological medium. To explore the mechanism of their chemotherapeutic effect, we studied their role in proliferation in the HCT116 human colon cancer cells. We correlated kinetic stability and cellular uptake data to their biological effects. Both bDMC and DAC impair correct spindles formation and induce a p53- and p21(CIP1/WAF1)- independent mitotic arrest, which is more stable and long-lasting for bDMC. A subsequent p53/p21(CIP1/WAF1)- dependent inhibition of G1 to S transition is triggered by Curcumin and DAC as a consequence of the mitotic slippage, preventing postmitotic cells from re-entering the cell cycle. Conversely, the G1/S arrest induced by bDMC is a direct effect of the drug and concomitant to the mitotic block. Finally, we demonstrate that bDMC induces rapid DNA double-strand breaks, moving for its possible development in anti-cancer clinical applications.
2009
- Development of new metal-chelating multi target drus derived from Curcumin
[Relazione in Atti di Convegno]
Ferrari, Erika; Pignedoli, Francesca; Lazzari, Sandra; Imbriano, Carol; Marverti, Gaetano; Saladini, Monica
abstract
With the aim to develop new anti-cancer approaches, which encompass therapies based on drug combinations, we are searching for innovative anti-tumor multi-targets treatments.1 In this research Curcumin represents our referring and starting point for the design of new derivatives. Curcumin, a natural occurring molecule, was shown to inhibit growth of several types of malignant cells and its biological activity was also related to its iron chelating ability.2 Recently curcumin proceeded onto clinical trials however its use is limited by a poor bioavailability. In order to improve curcumin water solubility and drug-delivery we have synthesized new derivatives which conjugate anti-proliferative effects with metal chelating capacity. They are able to reduce free iron level and to potentially deliver a chemotherapic metal ion such as Ga(III).
2009
- MALDI-TOF MS as a tool for rapid Identification of Low Protein Affinity Drug Fragments.
[Abstract in Atti di Convegno]
Genovese, Filippo; Lazzari, Sandra; G., Cruciani; Franchini, Silvia; S., Henrich; R. C., Wade; Venturelli, Alberto; Costi, Maria Paola
abstract
...
2009
- Microwave assisted synthesis of new β-diketo derivatives ligands
[Relazione in Atti di Convegno]
Ferrari, Erika; Lazzari, Sandra; Pignedoli, Francesca; Saladini, Monica; O., Verna; Corradi, Anna; Leonelli, Cristina; Rosa, Roberto; Veronesi, Paolo
abstract
The metal complexes of β-diketo derivatives and especially those of acetylacetone are well known and have been extensively studied. To improve the chelating ability of this molecule, we have introduced a further coordinative group. The designed compounds, which include a carboxylic group and the β-diketo moiety, are promising candidates as new metal ligands for pharmaceutical applications.
Classical synthetic strategy for the obtainment of these adducts requires a two step procedure consisting first in the SN2 reaction of methylenic group and second deprotection of ester derivatives in order to set the carboxylic function free.
Concerning the first step, traditional approach requires long reaction times and long work up procedures that lead to very poor product yields. Microwave (MW) irradiation at 2.45 GHz in closed vessels was exploited in this first synthetic step to take advantages from rapid heating rates thanks to the intrinsic volumetric and selectivity nature of MW heating.
Results in terms of reaction times and yields as well as possible future developments, will be discussed.
2009
- New Synthetic Glucosyl-Curcuminoids, and their 1Hand 13C NMR Characterization, from Curcuma longa L.
[Articolo su rivista]
Saladini, Monica; Lazzari, Sandra; Pignedoli, Francesca; Rosa, Roberto; F., Spagnolo; Ferrari, Erika
abstract
Turmeric extracts, among which curcumin and bisdemethoxycurcumin, are by far known for their therapeutic activities. In this study we propose easy and low cost synthetic pathways in order to obtain glucosyl-curcuminoids, safe and water soluble potential drugs and dyes, which may be implied in different fields ranging from pharmacology to food chemistry. The complete 1H and 13C NMR characterization of naturally occurring curcumin, bis-demethoxycurcumin and new synthetic glucosyl-curcuminoids is reported.
2009
- Synthesis and characterization of glucosyl-curcuminoids as Fe3+ suppliers in the treatment of iron deficiency
[Articolo su rivista]
Ferrari, Erika; Beatrice, Arezzini; Marco, Ferrali; Lazzari, Sandra; Pignedoli, Francesca; Ferdinando, Spagnolo; Saladini, Monica
abstract
The Fe3+ chelating ability of some curcumin glucosyl derivatives (Glc-H; Glc-OH; Glc-OCH3) is tested by means of UV and NMR study. The pK a values of the ligands and the overall stability constants of Fe3+ and Ga3+ complexes are evaluated from UV spectra. The only metal binding site of the ligand is the β-diketo moiety in the keto-enolic form; the glucosyl moiety does not interact with metal ion but it contributes to the stability of metal/ligand 1:2 complexes by means of hydrophilic interactions. These glucosyl derivatives are able to bind Fe3+ in a wide pH rage, forming complex species thermodynamically more stable than those of other ligands commonly used in the treatment of iron deficiency. In addition they demonstrate to have a poor affinity for competitive biological metal ions such as Ca2+. All ligands and their iron complexes have a good lypophilicity (log P > −0.7) suggesting an efficient gastrointestinal absorption in view of their possible use as iron supplements in oral therapy. The ligand molecules are also tested for their antioxidant properties in “ex vivo” biological system.
2009
- Synthesis, cytotoxic and combined cDDP activity of new stable curcumin derivatives
[Articolo su rivista]
Ferrari, Erika; Lazzari, Sandra; Marverti, Gaetano; Pignedoli, Francesca; Ferdinando, Spagnolo; Saladini, Monica
abstract
New curcumin derivatives are synthesized in order to improve chemical properties of curcumin. The aromatic ring glycosylation of curcumin provides more water-soluble compounds with a greater kinetic stability which is a fundamental feature for drug bioavailability. The glycosylation reaction is quite simple, low cost, with high yield and minimum waste. NMR data show that the ability of curcumin to coordinate metal ion, in particular Ga(III), is maintained in the synthesized products. Although the binding of glucose to curcumin reduces the cytotoxicity of the derivatives towards cisplatin (cDDP)-sensitive and -resistant human ovarian carcinoma cell lines, the compounds display a good selectivity since they are much less toxic against non-tumourigenic Vero cells. The combination of cDDP with the most active glycosyl-curcuminoid drug against both cDDP-sensitive and -resistant as well as against Vero cell lines is tested. The results show an improvement of cDDP efficacy with higher selectivity towards cancer cells than non-cancer cells. These studies indicate the need for developing new valid components of drug treatment protocols to cDDP-resistant cells as well.
2009
- Understanding the molecular mechanisms of Curcumin derivatives chemotherapic activity
[Relazione in Atti di Convegno]
Basile, Valentina; Ferrari, Erika; Lazzari, Sandra; Belluti, Silvia; Pignedoli, Francesca; Imbriano, Carol
abstract
....
2008
- Fe(III) containing complexes with beta-diketo derivatives for treatment of iron deficiency
[Relazione in Atti di Convegno]
Saladini, Monica; Ferrari, Erika; Lazzari, Sandra; Pignedoli, Francesca; F., Spagnolo
abstract
...
2008
- Merging disulphide bonds for drug design Interfering with a cancer key protein
[Abstract in Atti di Convegno]
Lazzari, Sandra; Venturelli, Alberto; G., Cruciani; Franchini, Silvia; S., Henrich; Genovese, Filippo; R. C., Wade; Costi, Maria Paola
abstract
...
2008
- Synthesis, chemical and biological studies on new Fe3þ-glycosilated b-diketo complexes for the treatment of iron deficiency
[Articolo su rivista]
Beatrice, Arezzini; Marco, Ferrali; Ferrari, Erika; Frassineti, Chiara; Lazzari, Sandra; Marverti, Gaetano; Ferdinando, Spagnolo; Saladini, Monica
abstract
A simple synthetic pathway to obtain glycosilated b-diketo derivatives is proposed. These compounds show a good iron(III) affinity thereforewe may suggest the use of their Fe3þ-complexes as oral iron supplements in the treatment of anaemia. The glycosilated compounds (6-GlcH, 6-GlcOH and 6-GlcOCH3) are characterized by means of spectroscopic (UV, 1H and 13C NMR) and potentiometric techniques; they have a good water solubility, are kinetically stable in physiological condition (t1/2 > 100 h) and show a low cytotoxicity also in high concentrations (IC50 > 400 mM). They are able to bind Fe3þ ion in acid condition (pHw2) forming complex species thermodynamically more stable than those of other ligands commonly used in the treatment of iron deficiency. The iron complexes show also a good kinetic stability both in acidic and physiological pH and have a good lypophilicity (log P > 0.7) that suggests an efficient gastrointestinal absorption in view of their possible use in oral therapy. In addition they demonstrate a poor affinity for competitive biological metal ion such as Ca2þ, and in particular 6-GlcOCH3 is able to inhibit lipid peroxidation.
2008
- Theoretical study on Curcumin: A comparison of calculated spectroscopic properties with NMR, UV–vis and IR experimental data
[Articolo su rivista]
Benassi, Rois; Ferrari, Erika; Lazzari, Sandra; F., Spagnolo; Saladini, Monica
abstract
The main target of this study is a high-level computational nalysis of Curcumin, employing DFT approach with two different sets of basis functions (B3LYP/6-31G* and B3LYP/6-311G**). Accurate quantum mechanical studies, both in vacuum and in methanol medium, are carried out with the aim to analyze the conformational equilibria, to find the most stable equilibrium structure and to define the nature of the molecular orbitals, fundamental to explain Curcumin binding characteristic. Our theoretical calculations, performed at B3LYP/6-31G* and B3LYP/6-311G** levels both in vacuum and in methanol medium,confirm that the keto-enolic forms are more stable than the di-keto one, whose extremely low population suggests that this structure should not influence Curcumin properties. Keto-enolic form C results the most stable, independently on calculation level and solvent (methanol) effect. HOMO and LUMO molecularorbitals are calculated for all the structures with the two sets of basis with very similar results. MEPs show that the negative charge is localized on the oxygen atoms, which, in the keto-enolic forms, point in the same direction enabling metal coordination.NMR, UV–vis and FT-IR experimental data are employed in the comparison with electronic and conformational properties of Curcumin resulting from theoretical calculations. The two different calculation levels (B3LYP/6-31G* and B3LYP/6-311G**) give very similar results.Good linear correlations between the experimental 1H and 13C NMR chemical shifts (dexp), in methanold4(MeOD) and DMSO-d6 (DMSO), and calculated magnetic isotropic shielding tensors (sigmacalc) are found (dexp = a *signacalc + b). A good prediction of UV–vis experimental maximum absorption (lambdamax) on the basisof conformer populations is obtained. A linear relation with a good correlation coefficient is observedplotting the FT-IR experimental wavenumbers vs. the calculated ones, allowing to predict FT-IR spectra.
2007
- 1H, 13C, 195Pt NMR study on platinum(II) interaction with sulphur containing Amadori compounds
[Articolo su rivista]
Ferrari, Erika; Grandi, Romano; Lazzari, Sandra; Marverti, Gaetano; Rossi, Cecilia; Saladini, Monica
abstract
AbstractThe NMR study on the interaction of Pt(II) with Amadori compounds is performed. The Amadori compounds are derived from the reaction of β-d-glucose with l-cystine leading to N,N′-di-(1-deoxy-β-fructos-1-yl)-l-cystine [FruCyscys], and with l-methionine leading to N-(1-deoxy-β-fructos-1-yl)-l-methionine [FruMet].The great instability of 2-(1,2,3,4,5-pentahydroxypentyl)-1,3-thiazolidine-4-carboxylic acid [GlcCys], formed by the condensation reaction of β-d-glucose and l-cysteine, prevents the formation of its Pt(II) complexes. Differently, FruMet well reacts with K2PtCl4 in 1:1 M/L molar ratio leading to the formation of [Pt(FruMet-N,S)Cl2], in which the Amadori compound coordinates the metal ion through nitrogen and sulphur atoms. FruMet originates also a solid trans complex [Pt(FruMet-N,S)2]Cl2. Its NMR solution study allowed to identify two isomers with respect to nitrogen and sulphur atoms: R,R and S,S.In [Pt2FruCyscysCl4] species, FruCyscys molecule links two Pt(II) ions giving rise to two pentaatomic N,S-chelate rings.
2007
- NMR study on Pt(II) interaction with Amadori compounds
[Articolo su rivista]
Ferrari, Erika; Grandi, Romano; Lazzari, Sandra; Saladini, Monica
abstract
AbstractHere we report the first evidence of Pt(II) interaction with Amadori compound [N-(1-deoxy-d-Fructos-1-yl)glycine (Fru-Hgly)]. The 1H and 195Pt NMR results show that complexation of Pt(II) by Fru-Hgly is strongly dependent on pH and reaction molar ratio. In 1/1 Pt/Fru-Hgly molar ratio, at acidic pH, the first coordination site is the carboxylic oxygen, while at physiological pH the anchoring group is the aminic one, in both cases the system slowly evolves towards an N,O chelating mode. In 1/2 Pt/Fru-Hgly molar ratio the only coordination site is nitrogen atom while the carboxylic oxygen is not involved in metal coordination.
2007
- Synthesis and characterization of new beta-diketo derivatives with iron chelating ability
[Articolo su rivista]
Benassi, Rois; Ferrari, Erika; Grandi, Romano; Lazzari, Sandra; Saladini, Monica
abstract
Here we report the synthesis, the characterization and a theoretical study on new glycosylated phenyl substituted beta-diketones; two classes of compounds are obtained according to the condensation reaction: central and side derivatives. Their iron(Ill) chelating ability is tested by means of UNT-visible (UV-vis), potentiometric and NMR techniques. The conformation of central derivatives does not allow any metal chelation, while side derivatives bind iron(111) through the P-dioxo moiety. The glycosyl moiety does not interact with metal ion but it helps to stabilize metal/ligand (1/3) complexes by means of hydrophylic interactions. The pK(a) of the ligands and the stability constants of their Fe(111) complexes are evaluated by means of UV-vis spectroscopy and potentiometry. A comparison with other iron-chelating agents, on the basis of lipophilicity and the pFe(III), is finally reported. (c) 2006 Elsevier Inc. All rights reserved.
2006
- Glucosyl curcuminoid derivatives: Fe(III) and Ga(III) chelating agents with anti-cancer properties
[Relazione in Atti di Convegno]
Ferrari, Erika; Frassineti, Chiara; Lazzari, Sandra; Marverti, Gaetano; Grandi, Romano; Saladini, Monica
abstract
...
2006
- Glucosyl curcuminoid derivatives: Fe(III) and Ga(III) chelating agents with anti-cancer properties
[Relazione in Atti di Convegno]
Ferrari, Erika; Frassineti, Chiara; Lazzari, Sandra; Marverti, Gaetano; Grandi, Romano; Saladini, Monica
abstract
...
2005
- Hg(II)-coordination by sugar-acids: Role of the hydroxy groups
[Articolo su rivista]
Ferrari, Erika; Grandi, Romano; Lazzari, Sandra; Saladini, Monica
abstract
A solution study on the ability of some derivatised sugars [glucuronic acid (GluA), galacturonic acid (GalA) and glucosaminic acid (GlNA)] to complex the Hg(II) ion is reported. The stability constants of the complex species were determined by potentiometric measurements while H-1 NMR experiments allow to define the coordination sites of sugar molecules. GluA coordinates the metal ion through the carboxylic oxygen and the O-4 hydroxyl group and is found to form more stable complexes with respect to GalA in which metal ligation is from the carboxylic oxygen and the O-5 ring oxygen. GlNA forms stable complexes chelating Hg(II) ion through carboxylic oxygen and the a-amino group. The ternary 2,2´-bipyridine containing systems were also investigated by means of potentiometric studies. The ML2 complexes were also isolated in the solid state and characterised by IR spectroscopy.
2005
- New conjugated beta-diketones as iron chelators for clinical use
[Relazione in Atti di Convegno]
Benassi, Rois; Ferrari, Erika; Grandi, Romano; Lazzari, Sandra; Saladini, Monica
abstract
...
2005
- New water soluble conjugated beta-diketones: potential iron-sequestering agents in treatment of Cooley’s anemia
[Relazione in Atti di Convegno]
Ferrari, Erika; Grandi, Romano; Lazzari, Sandra; Saladini, Monica
abstract
...
2004
- The reaction of Pt(II) with glucosyl-sulphur-containing amino acids
[Relazione in Atti di Convegno]
Ferrari, Erika; Lazzari, Sandra; Saladini, Monica
abstract
...