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放射增敏剂是一类能选择性地增加肿瘤乏氧细胞对放射敏感性的药物。它的开发和应用将大大提高肿瘤放疗的治愈率,自六十年代初以来,这类药物已取得很大进展。硝基咪唑类增敏剂发展概况 1963年Adams等提出化合物的放射增敏作用与其电子亲合性有关的论点,推动了亲电子性增敏剂的发展。其后,系统地研究了多种类型的化合物,如醌类、硝基苯类、硝基呋喃类和硝基咪唑类等,其中以硝基咪唑类作用最好。两只原为抗滴虫药的硝基咪唑类化合物,即甲硝唑(1)和米索硝唑
Radiosensitizers are a class of drugs that selectively increase the radiosensitivity of tumor cells that are hypoxic. Its development and application will greatly increase the cure rate of tumor radiotherapy and great progress has been made in these drugs since the early 1960s. Development of nitroimidazole sensitizers 1963 Adams et al proposed radiosensitization of compounds and their electronic affinity on the argument that promote the development of electrophilic sensitizers. Since then, many kinds of compounds have been systematically studied, such as quinones, nitrobenzenes, nitrofurans and nitroimidazoles, among which nitroimidazoles work best. Two of the original anti-trichomonas nitroimidazoles compounds, namely metronidazole (1) and misonidazole