Natural and synthetic indolocarbazole compounds have triggered considerable interest since the discovery in 1986 of the inhibitory properties of staurosporine toward protein kinase C (PKC). Later, it has been shown that indolocarbazole compounds may inhibit various kinases, such as cyclin dependent-kinases and/or topoisomerase I, someones behave only as DNA intercalators. In this review are presented various indolocarbazole compounds bearing a sugar moiety and their biological targets. The relevance of these targets to develop indolocarbazole compounds as potential antitumor agents is discussed.