engleski

Radioprotective and antitumor activity evaluation of newly synthesized adamantyl tenocyclidines.

Several adamantyl derivatives of thienyl phencyclidine (tenocyclidine, TCP)were newly synthesized and characterized ; adamantyl derivatives containing piperidine (TAPIP), pyrolidine (TAPIR) and morpholine (TAMORF) groups. Their biological activity was evaluated by in vitro testing of their effects on proliferative and reproductive ability (cytotoxicity) of human tumor cell strain and non-malignant mouse fibroblasts in culture. We also tested them for their radioprotective effect after ionising irradiation and as anticancer agents on the same human tumor cell strain. Comparing with tenocyclidine (TCP), adamantyl derivatives are less toxic and have outstanding radioprotective properties. These derivatives (especially TAMORF) increase apoptotic death of human malignant cells. Radiation modifying effect studied on C3Hf mice in vivo showed that the adamantyl derivatives of TCP have more enhanced radioperotective effect and they are less toxic than TCP itself. The present data are discussed and compared with those previously reported for structuraly related phenocyclidine derivatives.

adamantyl tenocyclidines; radioprotection; antitumor activity

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