Abstract: Among the various aspects of the present disclosure is the provision of compositions and methods for targeted treatment and detection of cancers. In particular, the present disclosure is directed to a compounds are from the benzofurazan, and nitrobenzofurazan family of compounds. The compounds inhibit tumor proliferation, induce regression of tumor growth or prevent tumor survival. In another embodiment, the compounds are labeled or conjugated with atoms or group of atoms that illuminate their distribution in cells and living organisms, the signals of which can be detected using imaging systems.