Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Synthesis of nοvel artemisinin dimers with polyamine linkers and evaluation of their potential as anticancer agents
Δημιουργός/Συγγραφέας:	Magoulas G.E. Tsigkou T. Skondra L. Lamprou M. Tsoukala P. Kokkinogouli V. Pantazaka E. Papaioannou D. Athanassopoulos C.M. Papadimitriou E.
Εκδότης:	Elsevier Ltd
Ημερομηνία:	2017
Γλώσσα:	Αγγλικά
ISSN:	0968-0896
DOI:	10.1016/j.bmc.2017.05.018
Άλλο:	PubMed ID: 28549888
Περίληψη:	The natural product artemisinin and derivatives thereof are currently considered as the drugs of choice for the treatment of malaria. At the same time, a significant number of such drugs have also shown interesting anticancer activity. In the context of the present research work, artemisinin was structurally modified and anchored to naturally occurring polyamines to afford new artemisinin dimeric conjugates whose potential anticancer activity was evaluated. All artemisinin conjugates tested were more effective than artemisinin itself in decreasing the number of MCF7 breast cancer cells. The effect required conjugation and was not due to the artemisinin analogue or the polyamine, alone or in combination. To elucidate potential mechanism of action, we used the most effective conjugates 6, 7, 9 and 12 and found that they decreased expression and secretion of the angiogenic growth factor pleiotrophin by the cancer cells themselves, and inhibited angiogenesis in vivo and endothelial cell growth in vitro. These data suggest that the new artemisinin dimers are good candidates for the development of effective anticancer agents.
Τίτλος πηγής δημοσίευσης:	Bioorganic and Medicinal Chemistry
Τόμος/Κεφάλαιο:	25
Τεύχος:	14
Σελίδες:	3756-3767
Θεματική Κατηγορία:	[EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry
Λέξεις-Κλειδιά:	Angiogenesis Artemisinin Breast cancer Conjugates Dimers Endothelial cells Polyamines
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Κάτοχος πνευματικών δικαιωμάτων:	© 2017 Elsevier Ltd
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο