eng URI http://hdl.handle.net/10795/3689 DNA καρκίνος The complex fac-[Re(CO)3(phendione)Cl] (1) (where phendione = 1,10-phenanthroline-5,6-dione) has been synthesized and fully characterized by UV–visible, FTIR, and NMR techniques. The DNA binding properties of 1 are investigated by UV-spectrophotometric (melting curves), covalent binding assay, CV (cyclic voltammetry), circular dichroism (CD) and viscosity measurements. Experimental data indicate that 1 fits into the major groove without disrupting the helical structure of the B-DNA in contrast to the free phendione which intercalates within the base pairs of DNA. Upon irradiation, complex 1promotes the cleavage of plasmid pBR322 DNA from supercoiled form I to nicked form II via a proton coupled electron transfer mechanism. This comes as a result of experimental data in anaerobic/aerobic conditions and in the presence of DMSO. The biological activities of 1 and its precursors [Re(CO)5Cl] and phendione are tested towards a series of cancerous cell lines as glioblastoma (T98G), prostate cancer (PC3) and breast cancer (MCF-7) as well as platelet activating factor (PAF)-aggregation. Moreover, all the aforementioned compounds are tested for their ability to modulate PAF-basic metabolic enzyme activities in preparations of rabbit leukolytes. The in vitro experiments indicate that phendione has a better antitumor effect than cisplatin whereas [Re(CO)5Cl] is a better PAF inhibitor than both the phendione ligand and 1. Moreover, for the first time it is indicated that [Re(CO)5Cl], with a IC50 of 17 nM is comparable to the widely used PAF receptor antagonists, BN52021 and WEB2170 with IC50 of 30 and 20 nM, respectively, whereas 1 affects PAF-catabolism. 39 pp. LOMv1.0 creator LOMv1.0 publisher LOMv1.0 Scientific Coordinator LOMv1.0 Project Executing Organisation 2014-02-06 Digital Library of the Operational Programme "Education and Lifelong Learning" abstract types Text Re(I) carbonyl Phendione DNA binding DNA photocleavage Anticancer activity PAF PAF-metabolism http://www.sciencedirect.com/science/article/pii/S0162013414000427 1292713 application/pdf http://repository.edulll.gr/edulll/bitstream/10795/3689/2/3689_1.121_%ce%94%ce%97%ce%9c_17_2_14.pdf URI http://hdl.handle.net/10795/3689 LOMv1.0creator 2016-06-21T09:15:49Z LOMv1.0validator 2016-06-21T09:15:49Z LOMv1.0 gre no no Copyright EYD-EPEDBM (Operational Programme "Education and Lifelong Learning")