Unit:
Κατεύθυνση Φαρμακευτική ΧημείαLibrary of the School of Science
Supervisors info:
Μικρός Εμμανουήλ, Καθηγητής Τμήμα Φαρμακευτικής ΕΚΠΑ,
Κωστάκης Ιωάννης, Αναπληρωτής Καθηγητής Τμήμα Φαρμακευτικής ΕΚΠΑ (επιβλέπων),
Παπαναστασίου Ιωάννης, Επίκουρος Καθηγητής Τμήμα Φαρμακευτικής ΕΚΠΑ
Original Title:
Σχεδιασμός και σύνθεση νέων αναλόγων της Flindersine ως πιθανοί αναστολείς της ΡΙΜ-1 κινάσης
Translated title:
Design and synthesis of novel Flindersine analogues as potential PIM-1 kinase inhibitors
Summary:
Protein kinases catalyze the enzymatic reaction of removing a phosphate group from ATP and covalently attaching it to a polar amino acid. Dysregulation of protein kinase activity results in pathological conditions, such as various types of cancer. Several studies in recent years have focused on PIM-1 kinase, which belongs to the family of serine/threonine protein kinases, and more specifically to the CAMK (calmodulin-dependent protein kinase) group. PIM-1 kinase is an attractive therapeutic target for anticancer drug discovery, as it is involved in the regulation of apoptosis, metabolism, cell cycle and migration. In more detail, the development of PIM-1 kinase inhibitors is aimed at treating the pathogenesis to which it contributes, such as myeloid leukemia and various types of cancer, such as prostate. The purpose of this thesis is the synthesis and design of analogs as potential inhibitors of PIM-1 kinase. The design of the derivatives synthesized and undergoing pharmacological evaluation was based on the results of previous experimental data that have taken place in our laboratory. More specifically, in our laboratory, analogs of Flindersine with inhibitory activity have been synthesized, such as, for example, 2,2-dimethyl-2,6-dihydro-5H-benzo[f]pyrano[3,2-c]quinoline-5-one, and based on these results, derivatives were designed and synthesized with the aim of optimizing binding to the active center of the enzyme, therefore a better pharmacological effect.
Main subject category:
Science
Keywords:
PIM-1 kinase, inhibitor, Flindersine, protein kinase, cancer, myeloid leukemia
File:
File access is restricted until 2026-05-26.
Master Myrto Gourli final'.pdf
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File access is restricted until 2026-05-26.
