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Design, synthesis and biological evaluation of new small molecule modulators of Arginine methyltransferases
(2011-02-21)
The methylation of arginine residues is a prevalent post-translational modification, found on both nuclear and cytoplasmic proteins, catalyzed by the protein arginine N-methyltransferase (PRMT) family of enzymes. To date ...
Design and synthesis of “small molecules” as antiviral and radiotracer agents
(2011-03-28)
The present Ph.D. project was divided into different work parts, in a way that helps to understand and define the goals of this project. In particular: I) Design, synthesis and evaluation of antiviral activity of Arbidol ...
The design and synthesis of novel N-heterocyclic compounds, and their evaluation of anti-cancer and anti-viral activity
(2014-05-21)
The thesis entitled “The design and synthesis of novel N-heterocyclic compounds, and their evaluation of anti-cancer and anti-viral activity" is divided into three chapters.
The title of the thesis clearly reflects the ...
Biophysical investigation of biomolecules in bio-membrane models
(2012-05-30)
Many drugs are available for the treatment of systemic or superficial mycoses,
but only a limited number of them are effective antifungal drugs, devoid of
toxic and undesirable side effects. Therefore there remains an ...
Design, synthesis and biological evaluation of new non-nucleosidic inhibitors od DNA methyltransferases
(2013-04-03)
The inactivation of tumor suppressor genes, which often results from epigenetic silencing associated with DNA hypermethylation, plays a pivotal role in the development of most forms of human cancer. Moreover, there are ...
Characterization and biological properties of Citrus industrial derivatives and waste products for the formulation of nutraceuticals
(2015-03-16)
Polyphenols are natural chemical compounds, common in higher plants as and particularly known and appreciated for their health properties. We focused attention on Citrus bergamia, Citrus sinensis, Mela annurca and Vitis ...
Analysis and evaluation of potential nutracentical milk and dairy products derived from the Centrale del latte di Salerno
(2015-03-16)
The main objective of my PhD has been focused to the analysis and characterization of milk and dairy products derived from “Centrale del Latte di Salerno” in order to assess their potential use as dietary supplements and ...
Design, synthesis, biological evaluation and binding studies of new small-molecule modulators of KDMs (lysine-specific demethylases)
(2017-03-27)
JHDMs (JmjC-domain-containing histone demethylases) are the largest class of demethylase enzymes, contain a Jumonji C (JmjC) domain and catalyze lysine demethylation of histones through an oxidative reaction that requires ...
Design and synthesis of modulators of apoptotic activity
(2016-03-23)
p53 is a transcription factor with tumour suppressor properties, which is able to induce mitochondrial apoptosis independently of its transcriptional activity. Analogues of the spiro[imidazo[1,5-c] thiazole-3,3′-indoline] ...
NMR-based metabolomic analysis of biological fluids to monitor relevant unsolved diseases
(2017-03-30)
Metabolomics and metabonomics encompass the comprehensive profiling of multiple metabolite
concentrations and their cellular and systemic fluctuations in response to drugs, diet, lifestyle,
environment, stimuli and genetic ...
Design, synthesis and biological evaluation of new small-molecule modulators of Protein Methyltransferases (PMTs)
(2016-04-21)
A large amount of evidences indicate that dysregulation of protein methylation is linked to the genesis and progression of several human diseases, including cancer. Therefore over the past years small-molecule modulators ...
Design, synthesis and biological evaluation of new small molecules with anti-inflammatory activity
(2015-03-18)
Per lipossigenasi (nota più comunemente con l'abbreviazione di LOX o LO) si intende una famiglia eterogenea di enzimi in grado di perossidare i lipidi e di causare l'ossigenazione di acidi grassi polinsaturi trasformandoli, ...
NMR study of protein-ligand interaction
(2015-03-11)
My PhD project was focused on the study of protein-ligands interactions using different NMR techniques. NMR has a long history in drug discovery and hit-to-lead optimization. Compared to many other biophysical techniques, ...
In vitro effects of bioactive extracts of local Italian cultivars: from molecular mechanisms to potential nutraceutical applications for consumers’ well-being
(2017-03-31)
Phytochemicals are non-nutritional compounds, naturally present in food and beverages, which exert
beneficial effects on human health. The present Doctorate Thesis evaluates the biological properties
of bioactive extracts ...
Synthesis of novel ligands for the stabilization of organometallic complexes having potential antitumor activity
(2016-05-04)
The design of new metal complexes as anticancer agents has received considerable interest in
recent years. Complexes of titanium (e.g.: titanocene dichloride), lanthanides complexes (e.g.:
texaphyrrins lanthanide) and ...
Synthesis, characterization and cytotoxicity studies of novel organo-metallic compounds
(2015-04-24)
Despite the discovery of cis-platin in the treatment of cancer there has
been a considerable exploration on the antitumoral activity of other
transition metal complexes. One of the main problems about the
application of ...
Design and synthesis of peptides involved in the inhibition of influenza virus infection
(2017-03-28)
The main purpose of the present research project was the identification of peptide capable of exercising potent anti-influenza activity. We identified bovine lactoferrin (bLf) as drug target, a multifunctional glycoprotein ...
Design and synthesis of new integrase inhibitors
(2017-03-28)
The viral enzyme integrase (IN) is essential for the replication of human immunodeficiency virus type 1 (HIV-1) and represents an important target for the development of new antiretroviral drugs. In this PhD project, we ...
Design, synthesis and biological evaluation of new anticancer and/or anti-inflammatory agents
(2017-03-22)
One of the main goal of modern medicinal chemistry is the development of new agents able to modulate biological targets involved in inflammation and cancer processes. In this context, my PhD project was focused on the ...