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Biological activity of benzimidazole and benzothizole 2,5-disubstituted furane derivatives

Among all known nitrogen heterocycles, benzimidazole and benzothiazole moieties have been recognized as important and well-known constituents of biologically important molecules in medicinal and pharmaceutical chemistry [1, 2]. Due to their wide range of biological activities, these heterocycles are still unavoidable structural motifs in the rational design of novel drugs. Newly designed and synthesized cyano, amidino and acrylonitrile 2, 5-disubstituted furane derivatives with either benzimidazole/benzothiazole nuclei have been evaluated for antitumor and antimicrobial activity, as well as for their interaction with ct-DNA. Compounds 5, 6, 8, 9 and 15 showed high potential antitumor activity on three human lung cancer cell lines and high activity against S. cerevisiae as a eukaryotic model organism. DNA study showed that all compounds dominantly bind inside the minor groove of AT-rich DNA.

amidines ; acrylonitriles ; benzimidazoles ; benzothiazoles ; furanes ; antitumor activity ; DNA binding

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