The incidence of cancer is rapidly increasing and malignancies have become the number two cause of deaths in the Western world after cardiovascular diseases. In particular, colon cancer represents one of the most frequent types of malignancy. Chemotherapy is, in addition to surgery and irradiation, still one of the main treatment options against this group of diseases. Here, several chemotherapeutic treatment modalities and anticancer compounds for the treatment of colon cancer are reviewed. In particular, a newer group of heterodinucleoside phosphates (dimers), consisting of two well known antimetabolites (5-FdUrd (5-Fluorodeoxyuridine) and Ara-C (Cytarabine)), are presented. These dimers were evaluated in several studies and might offer an additional option for the treatment of various malignancies, in particular colon carcinomas. The results are summarized in detail, as these dimers might have some significant advantages when compared with conventional regimens; they might be administered orally and might constitute an alternative treatment option for resistant tumors.