Synthetic studies on new 2-nitroimidazole derivatives with isoxazole and oxime structures for imaging tumor hypoxia

초록

Tumor hypoxia is the biological situation where tumor cells have been deprived of oxygen. The detection of hypoxia cell is important for treatment planning, such as in cases of cancer or myocardial ischemia. A number of isotopically labeled 2-nitroimidazole derivatives have been investigated as potential hypoxia markers. The nitro-aromatic classes of bio reductive derivatives were developed on the basis that the nitro functionality of the compound is able to be reduced under hypoxic conditions. Since 2-nitroimidazole heterocycles is the key structure in the field of imaging of hypoxia, it is important to introduce this 2-nitroimidazole ring for the discovery of new compounds. As part of discovering new imaging ligands, new 2-nitroimidaxole with isoxazole and oxime isomers containing fluorine and primary alcohol functionality were designed and synthesized. The basic concept, design and synthetic efforts of the target structures as possible hypoxia imaging ligands will be presented.