Unit:
Κατεύθυνση Σχεδιασμός και Ανάπτυξη νέων Φαρμακευτικών Ενώσεων - Φαρμακευτική ΧημείαLibrary of the School of Science
Author:
Kalampaliki Amalia
Supervisors info:
Ιωάννης Κ. Κωστάκης, Επίκουρος Καθηγητής, Τμήμα Φαρμακευτικής, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών
Original Title:
Σχεδιασμός και Σύνθεση υβριδίων ινδολίου και κιναζολίνης ως χημικών εργαλείων στη μελέτη της αντικαρκινικής δράσης
Translated title:
Design and Synthesis of Indole and Quinazoline Hybrids as Chemical Tools in the Study of Anticancer Activity
Summary:
Cancer is one of the major problems these days. In 2016, more than 1.7 million people died because of cancerous diseases. This made indispensable the synthesis of new drugs with intended anticancer activity. Some of the most well-known compounds include in their main domain the rings of indoles and quinazoline, which have been used as anticancer agents since the beginning. Very important compounds, secluded from plants with such characteristics and properties are Staurosporine and Rebeccamycin, as well as Rutaecarpine and Evodiamine and their analogues. Staurosporine and Rebeccamycin are indolocarbazole antibiotics with broad spectrum antitumor activity. Rebeccamycin and its analogues stabilize the DNA-topoisomerase cleavable complex and Staurosporine is one of the strongest known inhibitors of protein kinases. In addition, indoloquinazoline compounds, Rutaecarpine and Evodiamine possess anti-cancer activities both in vitro and in vivo by inhibiting proliferation, invasion and metastasis of a variety of tumor cell lines. Bis-indole derivatives have also been used for their kinases’ inhibitory properties and other distinct pathways of antitumor activity. The main goal of this project is to design and synthesize novel hybrids based on Staurosporine/Rebeccamycin, Rutaecarpine/Evodiamine and Bis-indole derivatives, which will include indole and quinazolinone groups in their main structure. These new synthesized compounds will be then substituted in order to evaluate the effect of them on topoisomerases' and/or protein kinases' inhibition, as well as on the tumor cell growth inhibition.
Main subject category:
Science
Other subject categories:
Pharmacy
Keywords:
indoles, quinazolines, cancer, kinases, topoisomerases, TDP
