Search Results - "PASSARELLA, Daniele"
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The 1,2,3-triazole ring as a bioisostere in medicinal chemistry
Published in Drug discovery today (01-10-2017)“…•Triazoles mimic different functional groups, resulting optimal bioisosteres for the synthesis of new active molecules.•Triazoles present a marked stability…”
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2
Cyrene: A Green Solvent for the Synthesis of Bioactive Molecules and Functional Biomaterials
Published in International journal of molecular sciences (15-12-2022)“…In the panorama of sustainable chemistry, the use of green solvents is increasingly emerging for the optimization of more eco-friendly processes which look to…”
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3
Cannabidiol as the Substrate in Acid-Catalyzed Intramolecular Cyclization
Published in Journal of natural products (Washington, D.C.) (23-10-2020)“…The chemical reactivity of cannabidiol is based on its ability to undergo intramolecular cyclization driven by the addition of a phenolic group to one of its…”
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4
Convenient Preparation and Spectroscopic Characterization of 7R-Hydroxymatairesinol
Published in Molecules (Basel, Switzerland) (26-09-2021)“…The preparation of 7R-HMR (allo-hydroxymatairesinol) is reported by: (a) NaBH4 kinetic reduction of 7R/7S diastereomeric mixture; and (b) epimerization of the…”
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5
Total Synthesis of (-)-Anaferine: A Further Ramification in a Diversity-Oriented Approach
Published in Molecules (Basel, Switzerland) (27-02-2020)“…The piperidine ring is a widespread motif in several natural bioactive alkaloids of both vegetal and marine origin. In the last years, a diversity-oriented…”
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6
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2023)“…EGFR is a protein kinase whose aberrant activity is frequently involved in the development of non-small lung cancer (NSCLC) drug resistant forms. The…”
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7
Recent Advances in SARS-CoV-2 Main Protease Inhibitors: From Nirmatrelvir to Future Perspectives
Published in Biomolecules (Basel, Switzerland) (01-09-2023)“…The main protease (M ) plays a pivotal role in the replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and is considered a highly…”
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8
Quantitative live cell imaging of a tauopathy model enables the identification of a polypharmacological drug candidate that restores physiological microtubule interaction
Published in Nature communications (23-02-2024)“…Tauopathies such as Alzheimer’s disease are characterized by aggregation and increased phosphorylation of the microtubule-associated protein tau. Tau’s…”
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9
Vincamine by synthesis and semi-synthesis
Published in Phytochemistry reviews (01-02-2021)“…This review summarizes the main strategies aimed at the total synthesis of vincamine and congeners. Then, our contribution in this field is presented: we…”
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Cannabidiol as Self-Assembly Inducer for Anticancer Drug-Based Nanoparticles
Published in Molecules (Basel, Switzerland) (23-12-2022)“…Cannabidiol (CBD) is a biologically active compound present in the plants of the family, used as anticonvulsant, anti-inflammatory, anti-anxiety, and more…”
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Synthesis and Preliminary Characterization of Putative Anle138b-Centered PROTACs against α-Synuclein Aggregation
Published in Pharmaceutics (11-05-2023)“…The search for disease-modifying agents targeted against Parkinson's disease led us to rationally design a small array of six Anle138b-centered PROTACs, , , ,…”
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12
Targeting Ovarian Cancer with Chalcone Derivatives: Cytotoxicity and Apoptosis Induction in HGSOC Cells
Published in Molecules (Basel, Switzerland) (25-11-2023)“…Ovarian cancer ranks as the eighth most prevalent form of cancer in women across the globe and stands as the third most frequent gynecological cancer,…”
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13
A small library of chalcones induce liver cancer cell death through Akt phosphorylation inhibition
Published in Scientific reports (16-07-2020)“…Hepatocellular carcinoma (HCC) ranks as the fifth most common and the second deadliest cancer worldwide. HCC is extremely resistant to the conventional…”
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Microtubule Alterations Occur Early in Experimental Parkinsonism and The Microtubule Stabilizer Epothilone D Is Neuroprotective
Published in Scientific reports (14-05-2013)“…The role of microtubule (MT) dysfunction in Parkinson's disease is emerging. It is still unknown whether it is a cause or a consequence of neurodegeneration…”
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15
Synthesis and Investigation of the G-Quadruplex Binding Properties of Kynurenic Acid Derivatives with a Dihydroimidazoquinoline-3,5-dione Core
Published in Molecules (Basel, Switzerland) (27-04-2022)“…G-quadruplexes are secondary structures originating from nucleic acid regions rich in guanines, which are well known for their involvement in gene…”
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Synthesis of (+)-Dumetorine and Congeners by Using Flow Chemistry Technologies
Published in Chemistry : a European journal (23-05-2011)“…An efficient total synthesis of the natural alkaloid (+)‐dumetorine by using flow technology is described. The process entailed five separate steps starting…”
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Discovery of a Novel Trifluoromethyl Diazirine Inhibitor of SARS-CoV-2 Mpro
Published in Molecules (Basel, Switzerland) (04-01-2023)“…SARS-CoV-2 Mpro is a chymotrypsin-like cysteine protease playing a relevant role during the replication and infectivity of SARS-CoV-2, the coronavirus…”
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18
Self-Assembly Nanoparticles of Natural Bioactive Abietane Diterpenes
Published in International journal of molecular sciences (01-10-2021)“…Different approaches have been reported to enhance penetration of small drugs through physiological barriers; among them is the self-assembly drug conjugates…”
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2-Hydroxyoleic Acid as a Self-Assembly Inducer for Anti-Cancer Drug-Centered Nanoparticles
Published in Pharmaceuticals (Basel, Switzerland) (09-05-2023)“…A potent nontoxic antitumor drug, 2-hydroxyoleic acid ( , 2OHOA) used for membrane lipid therapy, was selected as a self-assembly inducer due to its ability to…”
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Novel chemical probes for the investigation of nonribosomal peptide assembly
Published in Chemical communications (Cambridge, England) (2017)“…Chemical probes were devised and evaluated for the capture of biosynthetic intermediates involved in the bio-assembly of the nonribosomal peptide echinomycin…”
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