Κατεύθυνση Ανόργανη Χημεία και Τεχνολογία
Library of the School of Science

2017-07-19

2017

Konstantopoulos Timotheos

Μεθενίτης Κωνσταντίνος, Αναπληρωτής Καθηγητής, Τμήμα Χημείας, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών

ΣΥΝΘΕΣΗ ΚΑΙ ΧΑΡΑΚΤΗΡΙΣΜΟΣ ΤΟΥ ΓΛΥΚΟΖΥΛΙΩΜΕΝΟΥ ΠΑΡΑΓΩΓΟΥ ΤΗΣ 1,10-ΦΑΙΝΑΝΘΡΟΛΙΝΗΣ, (PDMalt). ΧΑΡΑΚΤΗΡΙΣΜΟΣ ΤΟΥ ΣΥΜΠΛΟΚΟΥ ΤΟΥ Cu(II) ME PDMalt. ΜΕΛΕΤΗ ΤΗΣ ΑΛΛΗΛΕΠΙΔΡΑΣΗΣ ΜΕ CT-DNA ΚΑΙ IN VITRO ΑΞΙΟΛΟΓΗΣΗ ΤΗΣ ΒΙΟΛΟΓΙΚΗΣ ΤΟΥ ΔΡΑΣΗΣ

Greek

SYNTHESIS AND CHARACTERIZATION OF GLYCOSYLATED DERIVATIVE OF 1,10-PHENANTHROLINE, (PDMalt). CHARACTERIZATION OF THE COMPLEX OF Cu(II) WITH PDMalt. STUDY OF THE INTERACTION WITH CT-DNA AND IN VITRO EVALUATION OF THEIR BIOLOGICAL ACTIVITY .

The aim of present thesis is the synthesis, characterization and study of Cu(II) complexes with 1,10-phenanthroline derivative, 2,9-di-{2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyox ane-3,4,5-trio}l-1,10-phenanthroline, as potential new anticancer agents. The corresponding Cu(II) complex was successfully synthesized and fully characterized by various spectroscopic methods (IR, NMR, MS, UV-vis). This complex is expected to be equally characterized by selective anticancer action of 1,10-phenanthroline in conjuction with the cytotoxicity of metallic center, targeting synergistic effectiveness. These metal complexes are designed with the method drug targeted delivery (DTD). According to this method, the initial ligand has a certain molecular group which is capable of delivering it to the targeted cell avoiding accumulation to healthy cells. In addition, this specific group gives to the ligand and the metal complex of it new characteristic properties. In this study, the group that was chosen for the modulation of the ligand is maltose, a disaccharide which gives to the initial molecule the desirable properties. Moreover, maltose as a sugar tends to interact with the DNA through its minor or major grooves (Groove Binding Affinity) and can easily be consumed by tumor cells due to alternate metabolic processes. In addition, their binding to CT-DNA was also been evaluated by UV-Vis spectroscopy, fluorescence, circular dichroism and viscometry. The data reveal that both the ligand and the complex strongly interact with CT-DNA, each one in different ways. The ligand interacts stabilizing the B- structure of DNA, via minor groove binding. On the other hand the most possible ways of interaction of the Cu (II) complex are the classic intercalation (or partial intercalation). Preliminary biological effects are encouraging since recruitment of cells was observed and increased cytotoxic activity of the Cu(II)-PDMalt on tumor cell lines of human osteosarcoma (MG63 Series).

Science

Chemistry

1,10- phenanthroline, copper (II), maltose, DNA, anticancer activity

Yes

4

Yes

79

142

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https://pergamos.lib.uoa.gr/uoa/dl/object/1725630