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Novel amino substituted derivatives of benzimidazo[1, 2-a]quinolines and benzo[b]thieno[2, 3-c]quinolones

One of the most important goals in medicinal chemistry is the development of new heterocyclic compounds with antitumor activity. Previously prepared derivatives of benzimidazo[1, 2-a]quinolines and benzo[b]thieno[2, 3-c]quinolones showed very good antitumor activity in vitro on a number of human tumor cell lines. Some of these compounds efficiently bind to double-stranded polynucleotides by intercalation.1-3 This work presents, as a part of our continuing research in the field of medicinal chemistry, the synthesis of novel amino-substituted derivatives of benzimidazo[1, 2-a]quinolines and benzo[b]thieno[2, 3-c]quinolones, as a potential biologically active agents. 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. Antitumor activity in vitro was tested on several human tumor cell lines. Interaction with ct-DNA of derivatives of benzimidazo[1, 2-a]quinolines was studied by using 4 different methods including thermal denaturation experiment, spectroscopic UV/Vis, fluorimetric and CD titrations with ct-DNA. [1] Hranjec, M., Kralj, M., Piantanida, I., Sedić, M., Šuman, L., Pavelić, K., Karminski-Zamola, G., J. Med. Chem. 50 (2007) 5696. [2] Hranjec, M., Pavlović, G., Marjanović, M., Kralj, M., Karminski-Zamola, G., Eur. J. Med. Chem. 45 (2010) 2405. [3] Jarak, I. ; Kralj, M. ; Šuman, L. ; Pavlović, G. ; Dogan, J. ; Piantanida, I. ; Žinić, M. ; Pavelić, K. ; Karminski-Zamola, G. J. Med. Chem. 2005, 48, 2346-2360.

benzimidazo[1; 2-a]quinolines; benzo[b]thieno[2; 3-c]quinolones; amino-substituted derivatives; antitumor activity; interaction with ct-DNA

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