A5055679259- Metal complexes synthesis and properties
- Ferrocene Chemistry and Applications
- Organometallic Compounds Synthesis and Characterization
- Organoselenium and organotellurium chemistry
- Microbial metabolism and enzyme function
- Asymmetric Hydrogenation and Catalysis
- Organometallic Complex Synthesis and Catalysis
- Inorganic Chemistry and Materials
- Redox biology and oxidative stress
- Organic Chemistry Cycloaddition Reactions
- Biochemical and Structural Characterization
- Chemical Thermodynamics and Molecular Structure
- Peptidase Inhibition and Analysis
- Toxin Mechanisms and Immunotoxins
- DNA and Nucleic Acid Chemistry
- HER2/EGFR in Cancer Research
- ATP Synthase and ATPases Research
- Free Radicals and Antioxidants
- Metalloenzymes and iron-sulfur proteins
- Inflammatory mediators and NSAID effects
- Trace Elements in Health
- Antimicrobial Peptides and Activities
- Chronic Myeloid Leukemia Treatments
- RNA and protein synthesis mechanisms
- Click Chemistry and Applications
University of Pisa
2022-2025
Background/Objectives: The ability of bacteria to form biofilms makes them more tolerant traditional antibiotics. Given the lack new antibiotic development, drug repurposing offers a strategy for discovering treatments. Auranofin (AF), gold-based compound indicated treatment rheumatoid arthritis, shows promising antibacterial activity. This study investigates antimicrobial and antibiofilm activity AF its two derivatives in which thiosugar ligand is replaced by acetylcysteine (AF-AcCys) or...
FETPY, an organo-diiron(I) complex, showed strong cytotoxicity across a panel of human and mouse cancer cell lines, combined with outstanding selectivity compared to nonmalignant cells. Enhanced iron uptake in aggressive, low-differentiated caused membrane lipid peroxidation, which resulted ferroptosis ovarian FETPY induced significant morphological changes murine B16–F1 B16–F10 melanoma cells, leading senescence and/or trans-differentiation into Schwann-like thus significantly reducing...
While gold nanoparticles (AuNPs) should allow the delivery of surface immobilized drugs to intended target tissues via bloodstream, their interactions with plasma proteins may induce aggregation and thus impede an effective chemotherapeutic agents tissues. The deliberate treatment AuNPs has potential overcome this inherent limitation. To probe between treated in blood plasma, we employed a size-exclusion chromatography (SEC)-based metallomics tool together transmission electron microscopy...
Cisplatin (CisPt), a platinum-based chemotherapeutic widely used in the treatment of various cancers, has multiple mechanisms action, including nuclear DNA (nDNA) and mitochondrial (mDNA) damage cytoskeletal perturbations affecting, turn, membrane transporter activity. CisPt binding to proteins enzymes may modulate its biochemical mechanism action is associated with cancer cell resistance drug. In this work, we investigate interaction between cisplatin angiogenin (Ang), protein strongly...
Auranofin (AF, hereafter) is an orally administered chrysotherapeutic agent approved for the treatment of rheumatoid arthritis that being repurposed various indications including bacterial infections. Its likely mode action involves impairment TrxR system through binding pharmacophoric cation [AuPEt3]+. Accordingly, a reliable strategy to expand medicinal profile AF replacement thiosugar moiety with different ligands. Herein, we aimed prepare analogue bearing acetylcysteine ligand (AF-AcCys,...
A variety of therapies are based on cytotoxicity induced via hampering the DNA and/or RNA homeostasis. The metallodrugs' forerunner, cisplatin, is exemplificative tremendous biological effects nucleobase targeting, and a large body researches to discover novel metallodrugs. In this paper, DFT approaches were employed investigate structure, stability electronic properties complexes formed by [Et3PAu]+ metal fragment generated auranofin -or its derivatives- DNA/RNA nucleobases. Therefore,...
Ammonium trichloro (dioxoethylene-O,O') tellurate (AS101) is a potent immunomodulator prodrug that, in recent years, entered various clinical trials and was tested for variety of potential therapeutic applications. It has been demonstrated that AS101 quickly activates aqueous milieu, producing TeOCl3-, which likely represents the pharmacologically active species. Here we report on study activation process two its analogues. After synthesis characterization derivatives, have carried out...
Since the serendipitous discovery of cisplatin, thousands inorganic molecules have been synthesized in search new drugs endowed with powerful anticancer activity and safe profile. As matter fact, this "magic" desired combination to date remains unmet. On other side, after only two additional platinum-based -that substantially designed as cisplatin-like molecules- approved at global level, i.e., carboplatin oxaliplatin. Accordingly, here, we try summarize highlight some relevant reasons for...
A variety of therapies are based on cytotoxicity induced via hampering the DNA and/or RNA homeostasis. The metallodrugs’ forerunner, cisplatin, is exemplificative tremendous biological effects nucleobase targeting, and a large body researches to discover novel metallodrugs. In this paper, DFT approaches were employed investigate structure, stability electronic properties complexes formed by [Et3PAu]+ metal fragment generated auranofin -or its derivatives- DNA/RNA nucleobases. Therefore,...
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AS101 (Ammonium trichloro (dioxoethylene-O,O') tellurate) is an important hypervalent Te-based prodrug. Recently, we started a systematic investigation on with the aim to correlate its promising biological effects as potent immunomodulator drug multiple medicinal applications and specific chemical properties. To date, substantial agreement rapid conversion of initial species into corresponding TeOCl
Multinuclear complexes are metal compounds featured by adjacent bound centers that can lead to unconventional reactivity. Some M
Auranofin ([1-(thio-κS)-β-D-glucopyranose-2,3,4,6-tetraacetato](triethylphosphine)-gold) is a leading gold-based drug clinically used to treat arthritis. In the last years, it entered various reprofiling programs, and has been found promising against forms of tumor, including ovarian cancer. Evidence showed as its antiproliferative profile mainly depends on inhibition thioredoxin reductase (TrxR), being this mitochondrial system main target. context, we report here synthesis biological...
Inorganic drugs are capable of tight interactions with proteins through coordination towards aminoacidic residues, and this feature is recognized as a key aspect for their pharmacological action. However, the "protein metalation process" exploitable solving phase problem structural resolution. In fact, use inorganic bearing specific metal centers ligands to drive binding desired portions protein target could represent very intriguing fruitful strategy. context, theoretical approach may...