Affiliation: Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
At present cancer treatment is still a confusing problem. Great progress has been made in anti-tumor agents since a series of small molecules are approved by FDA as anti-tumor drugs. Nitroimidazoles is a kind of radiosensitizer with multiple bioactivities used in cancer treatment since 1950s. In this review, we focus on the development of nitroimidazoles as radiosensitizer, bio-reductive prodrug and other types of anti-tumor agents for cancer therapy, and the mechanism of acting as anti-tumor agents. Finally, we also discuss the prospect and developmental trend of nitroimidazoles as anti-tumor agents.