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 1 promotes 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) 5 Cl] 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 enzymes activities in preparations of rabbit leukolytes. The in vitro experiments indicate that phendione has a better antitumor effect than cisplatin whereas [Re(CO) 5 Cl] is a better PAF inhibitor than both the phendione ligand and 1.Moreover, for the first time it is indicated that [Re(CO) 5 Cl], with a IC 50 of 17 nM is comparable to the widely used PAF receptor antagonists, BN52021 and WEB2170 with IC 50 of 30 and 20 nM, respectively, whereas 1 affects PAF-catabolism.
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