According to the results of studies revised and discussed in this paper, we identify the following highlights: (i) The low solubility and poor bioavailability of I3C and DIM limit their use as a medical treatment, so it is necessary to increase the research regarding pharmaceutic forms that improve these parameters, (ii) I3C and DIM have pro-apoptotic and antiproliferative effects and inhibit cell growth in pre-clinical and clinical cancer assays (Tables 2 and 3), (iii) Since I3C and DIM derivatives such as 5,5-Br2-DIM, the regulated cellular process associated with hallmarks of cancer, it could be essential to evaluate also these derivatives as anti-cancer agents, maybe in conjunct with DIM or I3C, and finally, (iv) The current evaluation of the anti-tumoral activities of DIM and I3C is generally based on mechanisms involving signalizing ways such as NF- B, Akt, Wnt, PI3K/Akt/mTOR, and AhR

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