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Synthesis, antitumor activity in vitro and interaction with ct-DNA of novel benzimidazo[1, 2-a]quinoline derivatives

One of the most important goals in medicinal chemistry is the development of new heterocyclic compounds with antitumor activity. Since the benzimidazole unit is the key building block for a variety of compounds which have crucial roles in the functions of biologically important molecules, there is a constant and growing interest over the past few years for the synthesis and biological studies of benzimidazole derivatives.1, 2 As a part of our continuing research in the field of medicinal chemistry, novel nitro- and amino substituted benzimidazole and benzimidazo[1, 2- a]quinoline derivatives as a potential biologically active agents were synthesized. For the preparation of targeted compounds, clasicall reactions of organic chemistry and photochemistry were used. All compounds were characterized by 1H, 13C NMR, IR, UV/Vis and fluorimetric spectroscopy. Preliminary interaction of amino-benzimidazo[1, 2- a]quinolines 5 and 8 with ct-DNA was studied by UV/Vis and fluorimetric spectroscopy and from obtained results we can conclude that this compounds showed strong interaction with ct- DNA. One of examinated compound showed increase of fluorescence intensity during the titration with ct-DNA and thus have possible application as fluorescent probe for nucleic acid detection in biomedicine. Antitumor activity in vitro of prepared compounds was tested on several human tumour cell lines.

Synthesis; antitumor activity in vitro and interaction with ct-DNA of novel benzimidazo[1; 2-a]quinoline derivatives

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