3－硝基－1，2，4－三唑类乏氧细胞放射增敏剂的构效关系

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。

STRUCTURE-ACTIVITY RELATIONSHIPS FOR 3-NITRO-1,2,4- TRIAZOLES AS HYPOXIC TUMOR CELL RADIOSENSTIZER

In order to search for effective radiosensitizer of hypoxic cell with low toxicity,a series of 5-bromo-,5-methy1-,and 5-unsubstituted-3-nitro-1,2,4-triazole-1- acetamides were synthesized and tested in vitro with HeLa S3 cells.The radiosensitlzing activity of 5-bromo-derivatives are more potent than those of corresponding 5-methyl-or 5- unsubstituted-1,2,4-triazole derivatives,but the chronic aerobic cytotoxicities are increased.Modification of the N1-acetamide side chain can also change the radiosensitizing activity and the lipophilicity.Among all the tested nitrotriazole derivatives,TA-101[2-(3- nitro-1-triazolyl)acetamide],may be a potential radiosensitizer because of its higher sensitizing activity and much lower lipophilicity.