Σχεδιασμός, σύνθεση και χαρακτηρισμός νέων εν δυνάμει εκλεκτικών αναστολέων πρωτεϊνικών κινασών, αναλόγων του φαρμακευτικού σκευάσματος της Νιλοτινίβης (Nilotinib), για τη θεραπεία νεοπλασιών (Master thesis)
Protein kinases are enzymes that play pivotal role in cell functions regulating many signal pathways by inducing ATP phosphorylation. Dysregulation of protein kinase and their receptors activity has been related to various diseases, including Chronic Myeoid Leukemia. Inhibition of these pathological protein kinases through small molecular weight compounds that compete the ATP binding site in the kinase active core is found to contribute in the treatment of the disease symptoms. For this reason, there is great interest in the scientific community for the synthesis and development of new more potent protein kinase inhibitors, acting selectively in the pathological protein kinase. Imatinib (Gleevec) is the first selective inhibitor who antagonizes the ATP binding site in the pathological Bcr-Abl tyrosine kinase in the treatment against Chronic Myeloid Leukemia (CML). Nilotinib was designed as a second generation selective Bcr-Abl kinase inhibitor and exhibits greater inhibitory activity compared to Imatinib. New compounds, Nilotinib analogues/derivatives, were synthesized in the laboratory, as a result of molecular modeling and it is possible to act more effectively on the protein kinases targets, aiming at their selective inhibition. These modifications on the original pharmaceutical compounds were targeted and were about the the last phenyl ring, where natural and non natural amino acids that increase the hydrogen bonds and the aromatic ability were attached. All new compounds were fully characterized (1H NMR, 13C NMR, MS).
|Institution and School/Department of submitter:||Πανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείας|
|Subject classification:||Κινάσες πρωτεινών|
|Appears in Collections:||Διατριβές Μεταπτυχιακής Έρευνας (Masters)|
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|Μ.Ε. ΒΟΥΛΓΑΡΗ ΠΗΝΕΛΟΠΗ 2017.pdf||8.12 MB||Adobe PDF||View/Open|
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