Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents

Abstract

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C1-C10 alkyl or haloalkyl; R′ and R″ are each independently C1-C10 alkyl; R1 is CH3; and X is O; or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.

Dependencies are inferred from the claim text.