Unit:
ΠΜΣ με ειδίκευση ΣΥΝΘΕΤΙΚΗ ΦΑΡΜΑΚΕΥΤΙΚΗ ΧΗΜΕΙΑLibrary of the School of Science
Author:
Παρασκευάς Κωνσταντίνος
Supervisors info:
Ιωάννης Κ. Κωστάκης Επίκ. Καθηγητής
Original Title:
Σχεδιασμός και σύνθεση νέων δισυποκατεστημένων πυριμιδο[4,5-d]πυριμιδινών ως πιθανών EGFR αναστολέων
Translated title:
Design and synthesis of novel disubstituted pyrimido[4,5-d]pyrimidines as potent EGFR inhibitors
Summary:
Protein kinases are targets for treatment of numerous diseases, including
cancer. One such protein is EGFR (Epidermal Growth Factor Receptor), which
belongs to the family of transmembrane receptors ErbB with intrinsic tyrosine
kinase activity. EGFR is involved in normal growth and shaping of cells and
tissues. However function abnormalities of EGFR associate with increased cell
proliferation and excessive angiogenesis and that is why its mutant subtypes
are found in many types of cancer as in glioblastoma, non-small cell lung
carcinoma (NSCLC), breast cancer, etc. One of the most successful
pharmacological approaches that has been developed so far for the inhibition of
EGFR includes the use of small molecules capable of inhibiting tyrosine kinases
(tyrosine kinase inhibitors-TKIs). 4-aminoquinazolines like gefitinib
(Iressa®), erlotinib (Tarceva®) and vandetanib (Caprelsa®) act in such way and
have shown remarkable efficacy in clinical phase III. Based mainly on this
class of compounds, in this thesis we report the design and synthesis of
disubstituted pyrimido[4,5-d]pyrimidines as potential antitumor agents, with
EGFR inhibitory activity.
Keywords:
EGFR, VEGFR, Kinases, Pyrimidines, Cancer
Number of references:
178
