1,2,4-Triazine N-oxide and N,N '-dioxide derivatives: Studies as potentialhypoxic cytotoxins and DNA binder

1,2,4-Triazine N-oxide and N,N'-dioxide derivatives were synthesized in ord er to obtain compounds as potential selective hypoxic cell cytotoxins. All the compounds were tested for their cytotoxicity in oxia and hypoxia and so me of them for their capacity to DNA-interaction in oxia. They proved to be less active in hypoxic conditions than the parent compound, tirapazamine ( 3-aminobenzo[1,2-e]1,2,4-triazine N-1,N-4-dioxide). However, derivatives 6, 9, and 10 developed signifrcant: affinity for DNA in oxic conditions. The electrochemical properties revealed that the lack of hypoxic - cytoxicity w as clearly related with their poor bioreductive characteristics.