Novel functionalized 2-phenylindole derivatives, their derived imidazole-2-thione and 1,2,4-triazine-3-thione compounds were synthesized. The bicyclic compounds thiazoloimidazole and thiazolotriazine compounds in addition to their arylidine derivatives were also prepared. Furthermore, thioglycoside as well as sugar hydrazone derivatives of the imidazolylindole system were synthesized. A number of the prepared compounds were screened against four cancer cell lines and compounds 2, 3a and 10 showed high cytotoxic activities. The imidazolylindol-3-one derivatives 3a showed significant cytotoxic effect against breast adenocarcinoma cell line with IC50 that is not too different from the reference drug.
Key words: 2-Phenylindole, Imidazole, Triazine, Glycosides, Cytotoxic, Breast adenocarcinoma.
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