engleski

Biochemical and spectroscopic characterization of quinolylmethylphosphonate complexes

Following the discovery of the cytostatic activity of cisplatin and its analogues, there is a continuing interest in the development of new platinum-based anticancer drugs with improved cytotoxicity and therapeutic properties. The studies on this type of compounds included also the substitution of platinum by its homologue palladium with similar coordination behavior in order to investigate the effects of the metal on the structural and biochemical properties of the complexes. Our systematic study is directed to palladium and platinum complexes of quinoline and aniline-based alkyl phosphonates as an effort to obtain metal complexes with potential antitumor and antiviral activity. We report here the synthesis, some spectroscopic properties (IR, 1H NMR, MS) and biological evaluation of new platinum(II) complexes of diethyl 8-quinolylmethylphosphonate (8-dqmp). The cytostatic activity of complexes was assayed in vitro on epidermoid human carcinoma KB, murine leukemia L1210/0 and human T-lymphoblast Molt4/C8 and CEM cell lines, and the antiviral assays were carried out in vitro in HEL, Vero and HeLa cell cultures infected with a variety of DNA and RNA viruses. The results obtained are compared with those of the palladium(II) chloride, bromide and acetate complexes of the same ligand and are discussed with respect to their structure-activity relationship. The greatest cell growth inhibitory effects display palladium dichloro adduct and acetate bridged dimmer, which may be regarded as having antitumor properties since their IC50 values are lower than 10 micromolar.

platinum(II) complex; aminophosphonate; cytostatic activity; antiviral activity

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