| Popis: |
Publisher Summary The discovery of the bactericidal activities of platinum complexes and their subsequent demonstration of the antitumor properties of this class of compounds stimulated the clinical development and utilization of cisplatin (cis-dichlorodiammine platinum II) in man. Although this material exhibits activity against several human malignancies, its therapeutic efficacy is compromised by the occurrence of severe dose-limiting toxic side effects. Predominant among these are nephrotoxicity, severe nausea and vomiting, myelotoxicity, and ototoxicity. The need for a less toxic antitumor platinum derivative is unequivocal. The growth inhibitory properties of the eight compounds have been compared against several transplantable rodent tumors and against a human epidermoid carcinoma of the bronchus (P246) grown in immune-deprived mice. The potential nephrotoxicities of these complexes have been assessed in the rat by following changes in blood urea levels: The histopathology of kidneys and other normal tissues has also been examined. In view of the similarities that exist between the mechanisms of action of platinum complexes and alkylating agents, the effects of the chosen platinum compounds on nuclear protein phosphorylation in the nuclei of tumor, kidney, and liver tissues. |
