Synthesis and Anticancer Activity of Novel 2-Phenylindole Linked Imidazolothiazole, Thiazolo-s-triazine and Imidazolyl-Sugar Systems

Abstract

Novel functionalized 2-phenylindole derivatives, their derived imidazolethione and 1,2,4-triazinethione were synthesized. The bicyclic compounds thiazoloimidazole and thiazolotriazine compounds in addition to their arylidine derivatives 5-8 were synthesized. Furthermore, a thioglycoside, as well as sugar hydrazone derivatives of the imidazolylindole system, were prepared. Some 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 superior to the reference drug, doxorubicin, against breast adenocarcinoma cell line.