Supervisors info:
: Καθηγητής κ. Αλέξιος-Λέανδρος Σκαλτσούνης, Καθηγητής κ. Βασίλειος Ρούσσης, Επίκουρος Καθηγητής κ. Νεκτάριος Αληγιάννης Επιβλέπων
Summary:
Deoxybenzoines, dihydrostilbenes and isoflavones, have been isolated from a
great number of plants and exhibited a wide range of significant biological
activities. Deoxybenzoins are considered to be precursors in synthesis of
isoflavones and show structural analogy with dihydrostilbenes, characteristics
that prompt us to synthesize analogues of deoxybenzoins, dihydrostilbenes and
isoflavones and study their biological activities concerning the tyrosinase
enzyme, the angiogenesis mechanism and the estrogen receptor,
Specifically, eleven (11) deoxyvenzoins were synthesised using Friedel-Crafts
acylation, six (6) dihydrostilbenes by catalytic hydrogenation under pressure
of the respective deoxybenzoins and eleven (11) isoflavones via formylation of
the initial deoxybenzoin followed by demethylation reaction and prenylation.
According to the biological activity studies of the above compounds, it is
worth noting that dihydrostilbene derivatives were proved to be potent
tyrosinase inhibitors and preliminary control of their activity on endothelial
cells, found that inhibit angiogenesis. Finally, a theoretical study of their
binding affinity to the estrogen receptor, took place.
Keywords:
Tyrosinase, Deoxybenzoins, Dihydrostilbenes, Isoflavones, Synthesis