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Synthesis and biological activity of novel N- substituted benzimidazole acrylonitriles

Small heteroaromatic molecules, like nitrogen- containing heterocycles play an important role in medicinal chemistry due to variety of their possible chemical, pharmacological and industrial applications. Benzimidazole structural motifs, as an important bioactive heterocyclic building block in medicinal chemistry, are widely incorporated in the structure of numerous natural or synthetic medical and biochemical molecules possessing versatile biological features.[1, 2] Within this work, we would like to present the synthesis and biological activity of novel N- substituted benzimidazole based acrylonitriles. For the synthesis of novel compounds we have used methods of classical linear organic synthesis as well as microwave assisted synthesis starting from aromatic benzaldehydes and substituted 1, 2- phenylenediamnies.[3] All newly prepared compounds were tested for their antiproliferative activity in vitro on nine human cancer as well as non cancerous cell lines. Some of compounds showed strong and selective antiproliferative activity in submicromolar range of IC50 concentrations. Additional experiments showed that some compounds did not affect normal cells. Mechanism of action studies demonstrated that two most active compounds inhibited the polymerisation of tubuline.

acrylonitriles, benzimidazoles, antiproliferative activity

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