engleski

Synthesis, microwave synthesis and antiproliferative activity of novel cyano and amidino benzazole amides

Cancer is a second leading cause of death in the Western World. Two potential targets for drug design in cancer are DNA and specific proteins like Topoisomerase I/II or Tyrosine Kinases. In the past few years a number of amido benzazole derivatives have been reported as inhibitors of above men-thioned proteins.[1, 2] We prepared in multistep synthesis [3] a series of new cyano and amidino benzazole amides by conventional and microwave synthesis. All compounds were characterized by IR, 1H and 13C NMR spectroscopy and elemental analysis. [1.] a) Das, J. ; Moquin, R. V. ; Lin, J. ; Liu, C. ; et al., Bioorg. & Med. Chem. Lett., 2003, 13, 2587. b) Abdel-Aziz, M. ; Matsuda, K. ; Otsuka, M. ; Uyeda, M. ; Okawara, T. ; Suzuki, K. ; Bioorg. & Med. Chem. Lett., 2004, 14, 1669. c) Yoshida, M. ; Hayakawa, I. ; Hayashi, N. ; Agatsuma, T. ; Oda, Y. ; et al., Bioorg. & Med. Chem. Lett., 2005, 15, 3328. [2.] a) Bürli, R. W. ; Jones, P. ; McMinn, D. ; Le, Q. ; Duan, J.-X. ; Kaizerman, J. A. ; Difuntorum, S. ; Moser, H. E. ; Bioorg. & Med. Chem. Lett., 2004, 14, 1259. b) Özden, S. ; Atabey, D. ; Yı ldı z, S. ; Göker, H. ; Bioorg.& Med. Chem., 2005, 13, 1587. [3.] a) Jarak, I. ; Kralj, M. ; Šuman, L. ; Pavlović, G. ; Dogan Koružnjak, J. ; Piantanida, I. ; Žinić, M. ; Pavelić, K. ; Karminski-Zamola, G. ; J. Med. Chem., 2005, 48, 2346. b) Jarak, I. ; Kralj, M. ; Piantanida, I. ; Šuman, L. ; Žinić, M. ; Pavelić, K. ; Karminski-Zamola, G. ; Bioorg. & Med. Chem., 2006, 14, 2859.

microwave synthesis; amides; benzazoles

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