A5052325016- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactivity of Heterocycles
- Cancer therapeutics and mechanisms
- Click Chemistry and Applications
- Synthesis and Reactions of Organic Compounds
- Bioactive Compounds and Antitumor Agents
- Chemical Reaction Mechanisms
- Synthesis and Characterization of Pyrroles
- Synthesis and pharmacology of benzodiazepine derivatives
- Synthesis of Organic Compounds
- Quinazolinone synthesis and applications
- Antimicrobial Peptides and Activities
- Chemical Reactions and Mechanisms
- Biochemical and Molecular Research
- Marine Sponges and Natural Products
- HIV/AIDS drug development and treatment
- Bacterial biofilms and quorum sensing
- Phenothiazines and Benzothiazines Synthesis and Activities
- Cyclopropane Reaction Mechanisms
- Organic Chemistry Cycloaddition Reactions
- Synthesis and Catalytic Reactions
- Synthesis of heterocyclic compounds
- Cancer Mechanisms and Therapy
University of Palermo
2016-2025
Humanitas University
2020
Amsterdam UMC Location Vrije Universiteit Amsterdam
2020
Regione Campania
2015
Atatürk University
2014
Izmir Bozyaka Eğitim ve Araştırma Hastanesi
2014
University of Tikrit
2014
Maulana Azad Medical College
2014
Institutul Național de Endocrinologie C.I. Parhon
2014
Fondazione IRCCS Istituto Nazionale dei Tumori
2013
Despite Imatinib (IM), a selective inhibitor of Bcr-Abl, having led to improved prognosis in Chronic Myeloid Leukemia (CML) patients, acquired resistance and long-term adverse effects is still being encountered.There is, therefore, urgent need develop alternative strategies overcome drug resistance.According the molecules expressed on their surface, exosomes can target specific cells.Exosomes also be loaded with variety molecules, thereby acting as vehicle for delivery therapeutic agents.In...
There is urgent need for new therapeutic strategies to fight the global threat of antibiotic resistance. The focus this Perspective on chemical agents that target most common mechanisms resistance such as enzymatic inactivation antibiotics, changes in cell permeability, and induction/activation efflux pumps. Here we assess current landscape challenges treatment at both bacterial community levels. We also discuss potential clinical application inhibitors add-on treatments serious...
Infectious diseases caused by antimicrobial-resistant strains have become a serious threat to global health, with high social and economic impact. Multi-resistant bacteria exhibit various mechanisms at both the cellular microbial community levels. Among different strategies proposed fight antibiotic resistance, we reckon that inhibition of bacterial adhesion host surfaces represents one most valid approaches, since it hampers virulence without affecting cell viability. Many structures...
Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that directly involved in altered cancer cell metabolism, resulting aggressiveness and resistance. Dichloroacetic acid (DCA) is the first PDK inhibitor has entered phase II clinical; however, several side effects associated with weak anticancer activity excessive drug dose (100 mg/kg) have led to its limitation clinical application. Building upon a molecular hybridization approach, small library of 3-amino-1,2,4-triazine...
A new series of nortopsentin analogs, in which the central imidazole ring natural lead was replaced by a 1,3,4-oxadiazole or 1,3,4-thiadiazole moiety, efficiently synthesized. The antiproliferative activity all synthesized derivatives evaluated against five pancreatic ductal adenocarcinoma (PDAC) cell lines, primary culture and gemcitabine-resistant variant. more potent compounds elicited EC50 values submicromolar-micromolar range, associated with significant reduction migration. Moreover,...
Pancreatic ductal adenocarcinoma (PDAC) is one of the main aggressive types cancer, characterized by late prognosis and drug resistance. Among factors sustaining PDAC progression, alteration cell metabolism has emerged to have a key role in proliferation, invasion, resistance standard chemotherapeutic agents. Taking into account all these urgency evaluating novel options treat PDAC, present work we reported synthesis new series indolyl-7-azaindolyl triazine compounds inspired marine...
In this study, we describe the synthesis of new nortopsentin analogues, 1H-pyrrolo[2,3-b]pyridine derivatives and their biological effects in experimental models diffuse malignant peritoneal mesothelioma (DMPM), a rare rapidly fatal disease, poorly responsive to conventional therapies. The three most active compounds, 1f (3-[2-(5-fluoro-1-methyl-1H-indol-3-yl)-1,3-thiazol-4-yl]-1H-pyrrolo[2,3-b]pyridine), 3f (3-[2-(1H-indol-3-yl)-1,3-thiazol-4-yl]-1-methyl-1H-pyrrolo[2,3-b]pyridine), 1l...
Isoindoloquinoxalines 4 and 5 were obtained by refluxing 2-(2′-aminoaryl)-1-cyanoisoindoles 3a−e in acetic or formic acid. All derivatives screened the National Cancer Institute (Bethesda, MD) for vitro one dose primary anticancer assay against a 3-cell line panel. Compounds 4a−e, panel of about 60 human tumor cell lines, showed remarkable antineoplastic activity; they had GI50 values low micromolar submicromolar range reached, case 4c, nanomolar concentrations on 88% 59 tested lines. Flow...
2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards panel 42 human tumor cell lines with mean IC50 values 1.54 μM 0.67 μM, respectively. Investigating xenografts an ex-vivo clonogenic assay revealed selective activity, whereas sensitive models scattered among various histotypes.