BW502U83, an arylmethylaminopropanediol (AMAP), showed to be partially cross-resistant in a P-glycoprotein-positive and in a P-glycoprotein-negative, doxorubicin-resistant cell line, while no cross-resistance was noticed in a cisplatin-resistant cell line. Interstrand cross-links were not observed, but BW502U83 induced extensive DNA strand breaks. In a feasibility study the effect of intra-arterially BW502U83 was tested. One patient with a hepatocellular carcinoma showed partial remission and signs of a tumorlysis syndrome, another patient with a hepatocellular carcinoma improved clinically. A patient with soft tissue sarcoma had stable disease. Transient increase in SGOT, SGPT and LDH were observed, but no systemic side effects.