Unit:
Τομέας ΦΑΡΜΑΚΕΥΤΙΚΗΣ ΤΕΧΝΟΛΟΓΙΑΣLibrary of the School of Science
Author:
Δημητρακούδη Σαπφώ-Μαρία
Supervisors info:
Καθηγητής κ. Αλέξιος-Λέανδρος Σκαλτσούνης, Καθηγητής κ. Βασίλειος Ρούσσης, Επίκουρος Καθηγητής κ. Νεκτάριος Αληγιάννης (Επιβλέπων)
Original Title:
Σχεδιασμός, σύνθεση και βιολογική αξιολόγηση αναλόγων 2-αρυλοβενζοφουρανίων
Summary:
2-arylbenzofurans have been the subject of extensive studies in the field of
medicinal chemistry because of their significant biological activity and the
classification of a large number of them to phytoestrogens. Design and
synthesis of such molecules have been the subject of this work due to the fact
that transformation of structure offers a high degree of diversity that has
proven useful in the search of new therapeutic targets. 20 2-arylobenzofurans
have been synthesized by the following three synthetic pathways; Sonogashira
coupling, as the main method of synthesis, and as alternative methods, Castro
reaction, a condensation reaction of copper aketylides with aryl-halogens, and
Suzuki reaction, a catalytic method utilizing boronic acids derivatives with
vinylethers. The synthesized coumpounds were studied as angiogenesis
inhibitors/inductors on endothelial cells and as tyrosinase inhibitors. Finally
we perform binding affinity simulation studies of our derivatives on the
estrogen receptor.
Keywords:
2-arylbenzofurans, Phytoestrogens, Estrogen receptor, Sonogashira coupling, Synthesis