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为了寻找毒性低、增敏作用强的乏氧细胞放射增敏剂,设计并合成了一系列5-溴-,5-甲基-,和5-未取代的3-硝基-1,2,4-三唑-1-乙酰胺类化合物,用HeLaS3细胞进行了体外试验。结果表明5-溴取代衍生物的增敏作用强于相应的5-甲基-或5-未取代的硝基三唑衍生物,但是它们的毒性亦增大。修饰1位乙酰胺侧链也可以改变化合物的增敏作用和亲脂性。在所测定的化合物中TA-101[2-(3-硝基-1-三唑基)乙酰胺]由于有高的增敏作用和低亲脂性,可能是一个有希望的放射增敏剂。
In order to find a hypoxic and sensitizing hypersensitive hypoxic cell radiosensitizer, a series of 5-bromo-, 5-methyl-, and 5-unsubstituted 3-nitro- 4-triazole-1-acetamide compounds were tested in vitro using HeLaS3 cells. The results show that the 5-bromo substituted derivatives have stronger sensitization than the corresponding 5-methyl- or 5-unsubstituted nitrotriazole derivatives, but their toxicity is also increased. Modification of the acetamide sidechain 1 can also alter the sensitization and lipophilicity of the compounds. Among the compounds tested, TA-101 [2- (3-nitro-1-triazolyl) acetamide] may be a promising radiosensitizer due to its high sensitization and low lipophilicity.