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Design and synthesis of modulators of apoptotic activity
(Universita degli studi di Salerno, 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] ...
Design, synthesis and biological evaluation of new anticancer and/or anti-inflammatory agents
(Universita degli studi di Salerno, 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 ...
Synthesis, characterization and cytotoxicity studies of novel organo-metallic compounds
(Universita degli studi di Salerno, 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 ...
In vitro effects of bioactive extracts of local Italian cultivars: from molecular mechanisms to potential nutraceutical applications for consumers’ well-being
(Universita degli studi di Salerno, 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 ...
Design, synthesis and biological evaluation of new small-molecule modulators of proein lysine methyltransferases (PKMTs)
(Universita degli studi di Salerno, 2018-04-20)
Histone lysine methyltransferases have crucial roles in a number of biological processes and human diseases by controlling gene expression and chromatin state. Within this family, the lysine methyltransferase G9a has emerged ...
Design and synthesis of peptides involved in the inhibition of influenza virus infection
(Universita degli studi di Salerno, 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, synthesis and biological studies of novel heterocyclic compounds as anticancer drugs
(Universita degli studi di Salerno, 2015-04-24)
Heterocyles are an essencial class of molecules, assuming a role in many aspect of
our life. Indeed heterocyclic nucleus is a common feature of several biomolecule and
bioactive compounds including agrochemical products ...
Design, synthesis, biological evaluation and binding studies of new small-molecule modulators of KDMs (lysine-specific demethylases)
(Universita degli studi di Salerno, 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 new integrase inhibitors
(Universita degli studi di Salerno, 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 ...
NMR-based metabolomic analysis of biological fluids to monitor relevant unsolved diseases
(Universita degli studi di Salerno, 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 and synthesis of “small molecules” as antiviral and radiotracer agents
(Universita degli studi di Salerno, 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 ...
Design, synthesis and biological evaluation of new small molecule modulators of Arginine methyltransferases
(Universita degli studi di Salerno, 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 ...
Analysis and evaluation of potential nutracentical milk and dairy products derived from the Centrale del latte di Salerno
(Universita degli studi 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 and biological evaluation of new non-nucleosidic inhibitors od DNA methyltransferases
(Universita degli studi di Salerno, 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 ...
The design and synthesis of novel N-heterocyclic compounds, and their evaluation of anti-cancer and anti-viral activity
(Universita degli studi di Salerno, 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
(Universita degli studi di Salerno, 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 ...
Biomolecular and biophysical approaches to interrogate epigenetic targets: a platform for drug discovery
(Universita degli studi di Salerno, 2016-04-20)
The term epigenetics refers to heritable changes in gene expression that do not involve changes in the DNA sequence. A large number of enzymes, which act mainly on histone tails and DNA, carries out epigenetic modifications, ...
Design and synthesis of bioactive small molecules by traditional and innovative methods
(Universita degli studi di Salerno, 2018-03-28)
My PhD research plan concerns the exploration of the structural requirements determining TRPM8 modulation. We prepared a series of N-substituted tryptamines and identified two compounds acting, respectively, as an activator ...
Design, synthesis, biological studies of new mitochondrial modulators improving neurological deficits in experimental models of Huntington's disease
(Universita degli studi di Salerno, 2017-03-22)
Design, synthesis and biological evaluation of new small-molecule modulators of Protein Methyltransferases (PMTs)
(Universita degli studi di Salerno, 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 ...