2-Nitroimidazol-5-ylmethyl as a potential bioreductively activated prodrug system: Reductively triggered release of the parp inhibitor 5- bromoisoquinolinone

Article abstract of DOI:10.1016/S0960-894X(99)00306-6

5-Chloromethyl-1-methyl-2-nitroimidazole reacted efficiently with the anion derived from 5-bromoisoquinolin-1-one to give 5-bromo-2-((1-methyl-2- nitroimidazol-5-yl)methyl)isoquinolin-1-one. Biomimetic reduction effected release of the 5-bromoisoquinolin-1-one. The 2-nitroimidazol-5-ylmethyl unit thus has potential for development as a general prodrug system for selective drug delivery to hypoxic tissues.