The Cu-catalyzed multicomponent ketone–amine–alkyne (KA2) reaction was combined with a Pauson–Khand cycloaddition to give access of unprecedented constrained spirocyclic pyrrolocyclopentenone derivatives following a DOS couple-pair... more
The Cu-catalyzed multicomponent ketone–amine–alkyne (KA2) reaction was combined with a Pauson–Khand cycloaddition to give access of unprecedented constrained spirocyclic pyrrolocyclopentenone derivatives following a DOS couple-pair approach. The polyfunctional molecular scaffolds were tested on the cyclopentenone reactivity to further expand the skeletal diversity, demonstrating the utility of this combined approach in generating novel spiro compounds as starting material for the generation of chemical libraries. The chemoinformatics characterization of the newly-synthesized molecules gave evidence about structural and physicochemical properties with respect to a set of blockbuster drugs, and showed that such scaffolds are drug-like but more spherical and three-dimensional in character than the drugs.
Research Interests:
Research Interests:
Research Interests:
Ad-proline peptidomimetic targeting MMP-2 and MMP-9 was identified from a pool of compounds following enzyme inhibition kinetics and Matrigel sponge assays, showing the capacity of blocking capillary network formationin vivo.
Research Interests:
The application of d-mannose as a multipurpose building block from the chiral pool enabled the diversity-oriented synthesis of an array of cyclic and bicyclic scaffolds with polyhydroxylated appendages with the aim to expand the skeletal... more
The application of d-mannose as a multipurpose building block from the chiral pool enabled the diversity-oriented synthesis of an array of cyclic and bicyclic scaffolds with polyhydroxylated appendages with the aim to expand the skeletal diversity in the panorama of glycopeptidomimetic compounds.
Research Interests:
The application of d-mannose as a multipurpose building block from the chiral pool enabled the diversity-oriented synthesis of an array of cyclic and bicyclic scaffolds with polyhydroxylated appendages with the aim to expand the skeletal... more
The application of d-mannose as a multipurpose building block from the chiral pool enabled the diversity-oriented synthesis of an array of cyclic and bicyclic scaffolds with polyhydroxylated appendages with the aim to expand the skeletal diversity in the panorama of glycopeptidomimetic compounds.
Research Interests:
Research Interests:
ABSTRACT Fragment-based drug discovery is a valuable tool in hit identification, as well as the combination of different small fragments showing a minimal binding activity against biological receptors or enzymes to give merged hits. A... more
ABSTRACT Fragment-based drug discovery is a valuable tool in hit identification, as well as the combination of different small fragments showing a minimal binding activity against biological receptors or enzymes to give merged hits. A high number of fragments on the same scaffold improve the probability to find a candidate showing single- or multi-target affinities. A rapid and versatile approach for synthesizing libraries of densely fragment-functionalized scaffolds is reported. Many fragments were assembled in few steps around a triazole ring starting from amino alcohols and other readily available building blocks. A binding assay against integrin alpha(v)beta(3) was used as a test-bed in order to demonstrate the potential of such an approach in hit discovery strategies.
Research Interests:
ABSTRACT
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Research Interests:
77 Journal of Organometallic Chemistry, 417 (1991) 7788 Elsevier Sequoia SA, Lausanne JOM 21897 Hydroformylation of olefins in the presence of dicobalt octacarbonyl: some considerations Franco Piacenti, Mario Bianchi, Piero Frediani,... more
77 Journal of Organometallic Chemistry, 417 (1991) 7788 Elsevier Sequoia SA, Lausanne JOM 21897 Hydroformylation of olefins in the presence of dicobalt octacarbonyl: some considerations Franco Piacenti, Mario Bianchi, Piero Frediani, Gloria Menchi Department of Organic ...
Research Interests:
Tetraruthenium dodecacarbonyl tetrahydride and some of its phosphine-substituted derivatives have been tested as homogeneous hydrogenation catalysts. The hydrogenation of cyclohexanone in the presence of H 4 Ru 4 (CO) 12 is first order... more
Tetraruthenium dodecacarbonyl tetrahydride and some of its phosphine-substituted derivatives have been tested as homogeneous hydrogenation catalysts. The hydrogenation of cyclohexanone in the presence of H 4 Ru 4 (CO) 12 is first order with respect to the catalyst concentration, ...
Research Interests:
Abstract The hydroformylation of pent-1-ene-5-d 3 in the presence of Ru 3 (CO) 12 H 4 Ru 4 (CO) 8 [(−)-DIOP] 2 under 750 atmosphere pressure of carbon monoxide gives a high percentage of the straight-chain isomer. Deuterium retention is... more
Abstract The hydroformylation of pent-1-ene-5-d 3 in the presence of Ru 3 (CO) 12 H 4 Ru 4 (CO) 8 [(−)-DIOP] 2 under 750 atmosphere pressure of carbon monoxide gives a high percentage of the straight-chain isomer. Deuterium retention is complete only under a ...
Research Interests:
Saturated monocarboxylic acids up to C 6 , several bicarboxylic acids and some of the corresponding anhydrides are hydrogenated in the homogeneous phase with H 4 Ru 4 (CO) 8 (PBu 3 ) 4 as catalyst to give the corresponding alcohols... more
Saturated monocarboxylic acids up to C 6 , several bicarboxylic acids and some of the corresponding anhydrides are hydrogenated in the homogeneous phase with H 4 Ru 4 (CO) 8 (PBu 3 ) 4 as catalyst to give the corresponding alcohols (present among the reaction products as ...
Research Interests:
Research Interests:
Research Interests:
The behaviour of the [Ru 2 (CO) 4 (CH 3 COO) 2 ] n /tributylphosphine/acetic acid system has been investigated as a function of reaction conditions and molar ratios of reactants. Tricyclohexylphosphine and triethylphosphite were also used... more
The behaviour of the [Ru 2 (CO) 4 (CH 3 COO) 2 ] n /tributylphosphine/acetic acid system has been investigated as a function of reaction conditions and molar ratios of reactants. Tricyclohexylphosphine and triethylphosphite were also used as ligands and investigation was extended to the ...
Research Interests:
The behaviour of the [Ru 2 (CO) 4 (CH 3 COO) 2 ] n /tributylphosphine/acetic acid system has been investigated as a function of reaction conditions and molar ratios of reactants. Tricyclohexylphosphine and triethylphosphite were also used... more
The behaviour of the [Ru 2 (CO) 4 (CH 3 COO) 2 ] n /tributylphosphine/acetic acid system has been investigated as a function of reaction conditions and molar ratios of reactants. Tricyclohexylphosphine and triethylphosphite were also used as ligands and investigation was extended to the ...
Research Interests:
Research Interests:
Research Interests:
Research Interests: Chemistry, Organic Chemistry, Medicinal Chemistry, Medicine, Humans, and 13 moreAnimals, Stereochemistry, Quantitative Structure Activity Relationship, Medicinal, Three Dimensional, Molecular Conformation, Biological activity, American Chemical Society, Pharmacophore, Steroid, CHO cells, Cricetinae, and Pharmacology and pharmaceutical sciences
Research Interests: Chemistry, Organic Chemistry, Medicinal Chemistry, Cell Adhesion, Positron Emission Tomography, and 15 moreMedicine, Angiogenesis, Humans, Melanoma, Cyclic peptides, Multimodal imaging, In Vivo, Glycine, Radiopharmaceuticals, Ligands, Integrin, Molecular probes, morpholine, Pharmacology and pharmaceutical sciences, and Human Umbilical Vein Endothelial Cells
Research Interests:
Research Interests:
Research Interests: Chemistry, Organic Chemistry, Medicine, Serotonin, Dopamine, and 15 moreCell line, Humans, Animals, Dat, Cocaine, Scaffold, Dopamine Transporter, Citalopram, Molecular Conformation, Recombinant Proteins, Ligands, Attention deficit hyperactivity disorder, CHO cells, Cricetinae, and Pharmacology and pharmaceutical sciences
Research Interests:
Research Interests: Stem Cells, Biology, Cell Biology, Medicine, Epithelial-Mesenchymal Transition, and 11 moreHumans, Endothelial Cells, Fibroblast, Transforming Growth Factor Beta, Triazoles, Vimentin, Molecular and Cellular Biochemistry, Integrin, Biochemistry and cell biology, Myofibroblast, and Transforming Growth Factor
Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to αvβ3 integrin with diverse potency, and selected (125)I-labeled compounds proved to interact in vitro and in vivo with αvβ3... more
Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to αvβ3 integrin with diverse potency, and selected (125)I-labeled compounds proved to interact in vitro and in vivo with αvβ3 integrin expressed by melanoma cells. Two (125)I-compounds containing either 2-aminobenzimidazole or 2-aminopyridine groups as the arginine bioisostere with the capacity to selectively bind cells of highly expressing αvβ3 melanoma xenografts were found using micro-SPECT imaging studies.
Research Interests:
ABSTRACT