… . 14. Synthesis and antitumor activity of 6-and 8-substituted imidazo [5, 1-d]-1, 2, 3, 5-tetrazinones and 8-substituted pyrazolo [5, 1-d]-1, 2, 3, 5-tetrazinones

E Lunt, CG Newton, C Smith, GP Stevens…

Index: Lunt, Edward; Newton, Christopher G.; Smith, Christopher; Stevens, Graham P.; Stevens, Malcolm F. G.; et al. Journal of Medicinal Chemistry, 1987 , vol. <2> 30, p. 357 - 366

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Citation Number: 48

Abstract

The systematic variation of the potent antitumor agent mitozolomide (1) is extended to cover alteration of substituents at positions 6 and 8 and to change the imidazo [5, 1-d]-1, 2, 3, 5- tetrazinone(6) skeleton to the isomeric pyrazolo-[5, 1-d]-1, 2, 3, 5-tetrazinone (17) skeleton. The series of eight 6-alkyl and 6-aralkyl derivatives of 1 showed optimal antitumor activity when the group was small or linear, but activity diminished as size and branching of this ...