A5085797426- Drug Transport and Resistance Mechanisms
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Nitric Oxide and Endothelin Effects
- Synthesis and biological activity
- Sulfur Compounds in Biology
- Research on Leishmaniasis Studies
- DNA and Nucleic Acid Chemistry
- Eicosanoids and Hypertension Pharmacology
- Malaria Research and Control
- Metal complexes synthesis and properties
- Trypanosoma species research and implications
- Energetic Materials and Combustion
- Bacterial biofilms and quorum sensing
- Synthesis of heterocyclic compounds
- Biochemical effects in animals
- Parasites and Host Interactions
- Luminescence and Fluorescent Materials
- Photodynamic Therapy Research Studies
- Computational Drug Discovery Methods
- Pharmacological Effects and Toxicity Studies
- Photochromic and Fluorescence Chemistry
- Glioma Diagnosis and Treatment
- Synthesis and Characterization of Heterocyclic Compounds
- Hormonal Regulation and Hypertension
University of Turin
2014-2025
Sapienza University of Rome
2024
Scuola Normale Superiore
2023-2024
National Research Council
2023-2024
Torino e-district
2018
Products 4 and 5, obtained by conjugation of doxorubicin with nitric oxide (NO) donor nitrooxy phenylsulfonyl furoxan moieties, respectively, accumulate in doxorubicin-resistant human colon cancer cells (HT29-dx), inducing high cytotoxicity. This behavior parallels the ability compounds to generate NO, detected as nitrite, these cells. Preliminary immunoblotting studies suggest that mechanism underlies cytotoxic effect could involve inhibition cellular drug efflux due nitration tyrosine...
Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the infectious disease responsible for highest number of deaths worldwide. Herein, 22 new N-oxide-containing compounds were synthesized followed in vitro and vivo evaluation their antitubercular potential against Mtb. Compound 8 was found to be most promising compound, with MIC90 values 1.10 6.62 μM active nonreplicating Mtb, respectively. Additionally, we carried out experiments confirm safety efficacy compound 8; orally...
ABSTRACT A novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a 14a to -f) benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) 7 8a -c) derivatives were synthesized, characterized, evaluated for in vitro activity against promastigote intracellular amastigote forms Leishmania amazonensis . The exhibited the ability generate nitric oxide at different levels (7.8% 27.4%). derivative was able increase nitrite production medium supernatant from murine macrophages infected...
A series of furoxan derivatives were studied for their ability to interact with P-gp and MRP1 transporters in MDCK cells overexpressing these proteins. 3-Phenylsulfonyl substituted furoxans emerged as the most interesting compounds. All them capable inhibiting P-gp, a few also MRP1. Substituents at 4-position 3-phenylsulfonylfuroxan scaffold able modulate selectivity intensity inhibition. In some cases, they reverted inhibitor activity, namely, potentiating dependent efflux. When compounds...
Abstract The design, synthesis, photochemical properties, and biological evaluation of a novel photoactivatable bichromophoric conjugate are reported. compound 1 , [4‐(4,4‐difluoro‐2,6‐diiodo‐1,3,5,7‐tetramethyl‐4‐bora‐3a,4a‐diaza‐ s ‐indacen‐8‐yl)‐ N ‐(3‐((4‐nitro‐3‐(trifluoromethyl)phenyl)amino)propyl)butanamide] combines 2,6‐diiodo‐1,3,5,7‐tetramethyl BODIPY derivative as singlet oxygen ( O 2 ) photosensitizer 4‐nitro‐3‐(trifluoromethyl)aniline (NOPD) nitric oxide (NO) photodonor, joined...
The synthesis and the physicochemical biological characterization of a series carnosine amides bearing on amido group alkyl substituents endowed with different lipophilicity are described. All synthesized products display carnosine-like properties differentiating from lead for their high serum stability. They able to complex Cu2+ ions at physiological pH same stoichiometry as carnosine. newly compounds highly significant copper ion sequestering ability capable protecting LDL oxidation...
Endophthalmitis is a rare, but serious, intravitreal inflammatory disorder that can arise after cataract surgery. The intracameral injection of 1 mg cefuroxime (CEF) followed by three-times daily antibiotic topical administration for week generally recognized as the routine method prophylaxis This procedure controversial because both low efficacy and adherence to therapy elderly patients. A unique slow release could solve these problems. objective present study was design ophthalmic...
A new series of (((R-oxy)carbonyl)oxy)methyl esters aspirin (ASA), bearing nitric oxide (NO) or hydrogen sulfide (H(2)S) releasing groups, was synthesized, and the compounds were evaluated as ASA co-drugs. All products quite stable in buffered solution at pH 1 7.4. Conversely, they all rapidly metabolized, producing NO/H(2)S moiety used for their preparation. Consequent on release, capable inhibiting collagen-induced platelet aggregation human platelet-rich plasma (PRP). The simple donor...
Antitumor chemotherapy remains one of the most important challenge medicinal chemistry. Emerging research in is focused on exploiting biochemical differences between cancer cell and normal metabolism order to reduce side effects increase antitumor therapy efficacy. The higher mitochondrial transmembrane potential cells compared not-transformed favors intra-mitochondrial accumulation cationic drugs former. This feature could be exploited allow selective delivery antineoplastic cells. In this...
P-Glycoprotein is a well-known membrane transporter responsible for the efflux of an ample spectrum anticancer drugs. Its relevance in management cancer chemotherapy increased view its high expression stem cells, population cells with strong tumor-promoting ability. In present study, series compounds were synthesized through structure modulation [4′-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-ylmethyl)biphenyl-4-ol] (MC70), modifying phenolic group lead compound. Among them, compound 5b...
P-glycoprotein (P-gp) is a well-known membrane transporter expressed in number of strategic biological barriers, where it exerts protective effect paramount importance. Conversely one the main causes multidrug resistance (MDR), being capable effluxing many chemotherapeutics. In development previous research, small library compounds was created conjugating diversely substituted furazan rings with MC70, P-gp inhibitor. These were assessed for their potency against and another (MRP1), apparent...
The use of nitric oxide (NO) as a signal for biofilm dispersal has been shown to increase the susceptibility many biofilms antibiotics, promoting their eradication. delivery NO can be achieved by using donors with different kinetics and properties release that influence efficacy control agents. In this study, three furoxan derivatives were evaluated. effects these donors, which have an advantageous pharmacological profile slower onset extended duration action, on Pseudomonas aeruginosa...
In the last years, research proofs have confirmed that hydrogen sulfide (H2S) plays an important role in various physio-pathological processes, such as oxidation, inflammation, neurophysiology, and cardiovascular protection; particular, protective effects of H2S diseases were demonstrated. The interest H2S-donating molecules tools for biological pharmacological studies has grown, together with understanding importance. Here we performed a comparative study series donor different chemical...
Hybrid products in which the dihydroartemisinin scaffold is combined with NO-donor furoxan and NONOate moieties have been synthesized studied as potential tools for treatment of cerebral malaria (CM). The designed were able to dilate rat aorta strips precontracted phenylephrine a NO-dependent mechanism. All hybrid compounds showed preserved antiplasmodial activity vitro vivo against Plasmodium berghei ANKA, comparable artesunate artemether. 10, selected additional studies, was capable...