Σχεδιασμός, σύνθεση και βιολογική αξιολόγηση αναλόγων 2-αρυλοβενζοφουρανίων

Postgraduate Thesis uoadl:1320273 490 Read counter

Unit:
Τομέας ΦΑΡΜΑΚΕΥΤΙΚΗΣ ΤΕΧΝΟΛΟΓΙΑΣ
Library of the School of Science
Deposit date:
2011-10-26
Year:
2011
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
Languages:
Greek
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
Index:
No
Number of index pages:
0
Contains images:
Yes
Number of references:
63
Number of pages:
154
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