A5069502576- Lanthanide and Transition Metal Complexes
- Radiopharmaceutical Chemistry and Applications
- Magnetism in coordination complexes
- Advanced MRI Techniques and Applications
- Radioactive element chemistry and processing
- Organometallic Complex Synthesis and Catalysis
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Analysis
- Medical Imaging Techniques and Applications
- Synthetic Organic Chemistry Methods
- Crystallization and Solubility Studies
- Oxidative Organic Chemistry Reactions
- Asymmetric Hydrogenation and Catalysis
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Cyclopropane Reaction Mechanisms
- Metal complexes synthesis and properties
- Catalysis for Biomass Conversion
- Chemical Synthesis and Characterization
- Supramolecular Chemistry and Complexes
- Amino Acid Enzymes and Metabolism
- Chemical Reactions and Isotopes
- Electron Spin Resonance Studies
- Carbohydrate Chemistry and Synthesis
- Bone health and treatments
- Mesoporous Materials and Catalysis
Bracco (Italy)
2014-2024
Mylan (Switzerland)
2021
Università degli Studi del Piemonte Orientale “Amedeo Avogadro”
2014
Princeton University
2006
University of Turin
2006
Bocconi University
2000
University of Milan
1989-1993
Abstract We report the synthesis of novel chelates Gd and 68 Ga with DPTA, DOTA, HP‐DOA3, as well AAZTA, a chelating agent developed by our research group. These agents were appropriately conjugated, prior to metal complexation, DB58, an RGD peptidomimetic, conformationally constrained on azabicycloalkane scaffold endowed high affinity for integrin α ν β 3 . Because is involved in neo‐angiogenesis solid tumors also directly expressed cancer cells (e.g. glioblastomas, melanomas) ovarian,...
The glutamine transporting system is up-regulated in tumor cells because cell proliferation requires the uptake of large quantities glutamine. It has been found that paramagnetic magnetic resonance imaging (MRI) reporter Gd-DOTAMA-C6-Gln, where residue covalently bound to Gd chelate through a C6 spacer, accumulates both "in vitro" and vivo" experiments. observation relaxivity cellular pellets does not increase with amounts entrapped taken as an indication internalization occurred receptor...
Bisalkylation of suitably protected l-glutamic acid and l-lysine derivatives with tert-butyl N-(2-bromoethyl)iminodiacetate 2, followed by deprotection the ω functional group affords N,N-bis[2-[bis[2-(1,1-dimethylethoxy)-2-oxoethyl]amino]ethyl]-l-glutamic 1-(1,1-dimethylethyl) ester 4 N2,N2-bis[2-[bis[2-(1,1-dimethylethoxy)-2-oxoethyl]amino]ethyl]-l-lysine 1,1-dimethylethyl 7. Such compounds feature a carboxylic or an amino group, respectively, which are available for conjugation suitable...
A novel Gd-DTPA derivative with a built-in sulfonamide (SA) was synthesized as contrast agent for MRI. The complex designed to selectively target the enzyme carbonic anhydrase. It is shown that longitudinal relaxation rates of aqueous solutions Gd-DTPA-SA in presence anhydrase increase significantly. binding constant determined be 15,000 ± 5,000 M–1. This value ensures substantial formation adduct at imaging concentrations Gd-DTPA-SA. interacts erythrocytes, presumably due high affinity...
A series of structurally different Gd(III) conjugates incorporating a bile acid moiety have been prepared. Polyaminopolycarboxylic ligands such as diethylenetriaminepentaacetic (DTPA) and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic (DOTA) selected chelating subunit for the ion. Cholic acid, cholylglycine, cholyltaurine incorporated moieties. In first generation complex is linked to carboxyl group cholic acid. Second feature attachment 3 position steroidic backbone Finally, in third...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTOpening of oxirane rings by the conjugate base pentacarbonyl(methoxymethylcarbene)chromium in presence boron trifluoride etherate: a general and improved synthesis pentacarbonyl(2-oxacyclopentylidene)chromium compoundsLuciano. Lattuada, Emanuela. Licandro, Stefano. Maiorana, Henriette. Molinari, Antonio. PapagniCite this: Organometallics 1991, 10, 3, 807–812Publication Date (Print):March 27, 1991Publication History Published online1 May...
The relaxivity of Gd(HP-DO3A) was studied as a function pH and buffer composition in order to identify the main factors observed relaxation enhancement due exchange coordinated hydroxyl proton. It established that paramagnetic time, T1M, proton is about 50% shorter than protons water molecule. control p K alcoholic -OH moiety ligand fundamental utilize enhanced under physio/pathologic conditions. A new derivative synthesized by replacing -CH3 group with -CF3 moiety. In this complex, becomes...
Complexes of Gd, Eu and Yb(III) have been prepared with a series heptadentate ligands related to the parent complex AAZTA, based on 6-methyl-6-aminoperhydrodiazepine moiety. For (RR) (RS)-diastereoisomers di-glutarate ligand, solution NMR studies revealed presence two major species that undergo water exchange rates at Gd differing by factor six. Comparison hydration states for Eu(III) complexes reveals each possesses bound molecules. The absence good correlation 1H pseudo-contact shifts Yb...
Purpose To dissect the contributions to longitudinal relaxivity (r 1 ) of two commercial contrast agents (CAs), Gd‐DOTA and Gd‐HP‐DO3A, synthesize/characterize a novel macrocyclic agent (Gd‐Phen‐DO3A) having superior r . Methods Longitudinal relaxation rates R CAs in saline with/without human serum albumin (HSA), ionized simulated body fluid (i‐SBF), viscous (v‐SBF), plasma were measured. Results have been interpreted evince main determinants observed values. In v‐SBF or presence HSA, is...
Abstract 3-Hydroxycholan-24-oic acid esters are easily converted into the corresponding 3-amino derivatives via Mitsunobu reaction with diphenylphosphoryl azide (DPPA) and Staudinger reduction PPh3/H2O of intermediate azido compound in THF.
Three novel BFCAs are obtained through an original protocol involving enzymatic hydrolysis as the key step.
Anchoring three picolinate units on a AMPED scaffold affords strongly pre-organized ligand for the formation of luminescent lanthanide complexes.
The Gd<sup>III</sup> complex of Ph-HP-DO3A shows the highest contribution to relaxivity by intramolecular proton exchange –OH group.
The synthesis of DOTA tris(phenylmethyl) ester 2, a new monoreactive derivative DOTA, is described. This versatile synthon can be easily coupled to compounds bearing an amino group and then deprotected monoamide under mild neutral conditions by catalytic hydrogenolysis. Accordingly, compound 2 has been used in the gadolinium complex containing two palmitic esters, which component mixed micelles as MRI contrast agents.
Two structurally constrained chelators based on a fused bicyclic scaffold, 4-amino-4-methylperhydro-pyrido[1,2-a][1,4]diazepin-N,N',N'-triacetic acids [(4R*,10aS*)-PIDAZTA (L1) and (4R*,10aR*)-PIDAZTA (L2)], were designed for the preparation of GaIII -based radiopharmaceuticals. The stereochemistry ligand scaffold has deep impact properties complexes, with unexpected [Ga(L2)OH] species being superior in terms both thermodynamic stability inertness. This peculiar behavior was rationalized...
The simple modification of the hydroxypropyl arm in Gd(HP-DO3A) complex allows to achieve an increased relaxivity by activation intramolecular catalysis proton exchange process.
Abstract Gd(III)‐complexes have been employed for more than twentyfive years as MRI contrast agents. In the last decade, considerations about potential toxicity of residual gadolinium in patients suffering from severe kidney diseases moved researchers to evaluate alternative solutions, among them Mn(II)‐complexes, shorten T 1 and achieve good image contrast. this article we report on synthesis a new Mn(II)‐chelate, endowed with deoxycholic acid residue designed interact reversibly serum...