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This thesis describes the first systematic investigation of the relationship between lipophilicity and reactivity on the one hand and cellular accumulation and cytotoxic activity on the other hand of a new class of oxaliplatin derivatives with different substituents at position 4 of the cyclohexane ring and different leaving ligands. Furthermore, the contribution of hCTR1 and hOCT1-3 on the influx of oxaliplatin was investigated. Information regarding the influence of oxaliplatin on the expression of these transporters, as well as on their localization inside cancer cells is still limited. In contrast to the studies conducted in the past, in this study no transfected cell lines were used.