Biological Evaluation of Novel Bicyclic Heteroaromatic Benzazole Derived Acrylonitriles: Synthesis, Antiproliferative and Antibacterial Activity

Within this manuscript we present the design, synthesis and biological evaluation of novel benzazole derived acrylonitriles bearing bicyclic heteroaromatic rings. Either benzimidazole, benzothiazole or imidazo[4,5- b ]pyridine scaffolds are linked via acrylonitrile linker with different bicyclic heteroaromatics. All newly prepared are evaluated for their in vitro antiproliferative activity on 8 human cancer cells as well as on three human lung cancer cell lines in MTS citotoxicity and in BrdU proliferative assays performed on 2D and 3D assay format. Majority of tested compounds showed weak activity with the exception of naphthyl substituted benzimidazole derivative 13 and benzothiazolyl substituted derivative 17 , both benzimidazole derived acrylonitriles. Also, as a promising compounds have proven to be imidazo[4,5- b ]pyridine derivatives 25 and 30 with selective activity against A549 cells. Furthermore, all compounds were tested for their antibacterial activity against nine bacteria strains and Saccharomyces cerevisiae . Only benzo[ b ]furan-2-yl substituted benzimidazole derivative 14 showed moderate activity.