Experimental Background and Early Clinical Studies with Imidazotetrazine Derivatives

A series of imidazotetrazine derivatives were synthesised by Stevens and colleagues in the late 70′s (1). The activity of one of these derivatives, mitozolamide (8-carbamoyl-3-(2-chloroethyl)imidazo[5-1-d]-1,2,3,5-tetrazin-4(3H)-one) was identified and the compound’s ability to cross link DNA confirmed (2, 3, 4).