A5041503491- Cancer therapeutics and mechanisms
- Synthesis and biological activity
- Beetle Biology and Toxicology Studies
- Alkaloids: synthesis and pharmacology
- Radical Photochemical Reactions
- Enzyme-mediated dye degradation
- Bioactive Compounds and Antitumor Agents
- Chemical Synthesis and Analysis
- Chemical synthesis and alkaloids
- Oxidative Organic Chemistry Reactions
- HIV/AIDS drug development and treatment
- Synthesis and bioactivity of alkaloids
- Phytochemical compounds biological activities
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- RNA Interference and Gene Delivery
- Advanced biosensing and bioanalysis techniques
- Catalytic C–H Functionalization Methods
- Microbial Natural Products and Biosynthesis
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthetic Organic Chemistry Methods
- Dendrimers and Hyperbranched Polymers
- Multicomponent Synthesis of Heterocycles
- Nitric Oxide and Endothelin Effects
- Plant chemical constituents analysis
Azienda Sanitaria Locale Viterbo
2024
Università degli Studi della Tuscia
2019-2023
Delft University of Technology
2022
Viterbo University
2020
A library of hybrid and dimer compounds based on the natural scaffold artemisinin was synthesized. These derivatives were obtained by coupling derivatives, artesunate, dihydroartemisinin with a panel phytochemical compounds. The novel artemisinin-based hybrids dimers evaluated for their anticancer activity cervical cancer cell line (HeLa) three complementary metastatic melanoma lines (SK-MEL3, SK-MEL24, RPMI-7951). Two artesunate eugenol tyrosol, one containing curcumin, emerged as most...
Stilbene and chalcone derivatives with biological activity against influenza A virus have been synthesized by self-, cross-, ring-closing metathesis procedures. The reactions were performed under environmentally friendly conditions using the second generation Hoveyda-Grubbs catalyst Aquamet SiPr after immobilization on Santa Barbara Amorphous mesoporous silicate SBA-15. Irrespective from experimental conditions, heterogeneous showed selectivity comparable than homogeneous counterpart for at...
Artesunic acid and artemisinin are natural substances with promiscuous anticancer activity against different types of cancer cell lines. The mechanism action these compounds is associated the formation reactive radical species by cleavage sesquiterpene pharmacophore endoperoxide bridge. Here we suggested topoisomerase 1 as a possible molecular target for improvement compounds. In this context, report that novel hybrid dimer derivatives artesunic artemisinin, bearing camptothecin SN38...
We report here the synthesis of novel thymine biomimetic photo-adducts bearing an alkane spacer between nucleobases and characterized by antimelanoma activity against two mutated cancer cell lines overexpressing human Topoisomerase 1 (TOP1), namely SKMEL28 RPMI7951. Among them, Dewar Valence showed a selectivity index higher than corresponding pyrimidine-(6-4)-pyrimidone cyclobutane counterpart were highest affinity towards TOP1/DNA complex as evaluated molecular docking analysis. The was...
Abstract A photochemoenzymatic halodecarboxylation of ferulic acid was achieved using vanadate‐dependent chloroperoxidase as (bio)catalyst and oxygen organic solvent sole stoichiometric reagents in a biphasic system. Performance selectivity were improved through phase transfer catalyst, reaching turnover number 660.000 for the enzyme.
Belladine
A library of five hybrids and six dimers dihydroartemisinin artesunic acid has been synthetized in a stereo-controlled manner evaluated for the anticancer activity against metastatic melanoma cell line (RPMI7951). Among novel derivatives, three showed antimelanoma cancer selectivity, being not toxic on normal human fibroblast (C3PV) line. dimers, one bearing 4-hydroxybenzyl alcohol as spacer no cytotoxic effect (CC50 >300 μM) high (IC50 =0.05 μM), which was two orders magnitude higher than...
Laccase-mediated intramolecular oxidative radical coupling of N-formyl-2-bromo-O-methylnorbelladine afforded a novel and isolable spirocyclohexadienonic intermediate galantamine. High yield conversion substrate were obtained in the presence redox mediator 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO). This laccase procedure, with an overall 34%, represents scalable environmentally friendly alternative to previously reported syntheses galantamine based on use potassium ferricyanide as...
Abstract A blue‐LED‐driven two‐liquid‐phase system has been set up for the in situ activation of horseradish peroxidase avoiding use hydrogen peroxide and drawbacks related to enzyme denaturation undesired radical side‐reactions. The photobiocatalytic was applied oxidative coupling natural synthetic coumarins bicoumarins, allowing obtain homodimers only one step, tedious protecting groups. Two C‐2 symmetric bicoumarins derived from scopoletin were synthesized first time. UV‐visible...
Current therapy against melanoma relies on surgical treatment or, in alternative, conventional drug therapy. Often these therapeutic agents are ineffective due to the development of resistance phenomena. For this purpose, chemical hybridization emerged as an effective strategy overcome resistance. In study, a series molecular hybrids were synthesized combining sesquiterpene artesunic acid with panel phytochemical coumarins. Cytotoxicity, antimelanoma effect, and cancer selectivity novel...
Abstract Vicinal halohydrins are key building blocks to produce bioactive molecules and drugs, especially if they can be obtained in enantiomerically pure form. In this study, we present a bi‐enzymatic sequence that allows obtain vic ‐halohydrins through photochemoenzymatic olefin hydroxy halogenation followed by lipase catalysed kinetic resolution. The absolute configuration of the resulting products was determined using Mosher's method